标签归档：hydrochloride

Kasugamycin hydrochloride(Synonyms: Ksg hydrochloride)

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天然产物 糖类和糖苷 Saccharides and Glycosides

Kasugamycin hydrochloride;(Synonyms: Ksg hydrochloride)

Kasugamycin hydrochloride (Ksg hydrochloride) 是一种既能结合 30s 和 70s 核糖体又不能结合 50s 亚基的抗生素。Kasugamycin hydrochloride (Ksg hydrochloride) 模拟 mRNA 核苷酸破坏 tRNA 结合并抑制典型翻译起始。

Kasugamycin hydrochloride(Synonyms: Ksg hydrochloride)

Kasugamycin hydrochloride Chemical Structure

CAS No. : 19408-46-9

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生物活性

Kasugamycin hydrochloride (Ksg hydrochloride) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin hydrochloride (Ksg hydrochloride) mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation[1][2].

分子量

415.82

Formula

C14H26ClN3O9
CAS 号

19408-46-9
中文名称

春雷霉素盐酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Schluenzen F, et al. The antibiotic kasugamycin mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation. Nat Struct Mol Biol. 2006 Oct;13(10):871-8.

    [2]. Schuwirth BS, et al. Structural analysis of kasugamycin inhibition of translation. Nat Struct Mol Biol. 2006 Oct;13(10):879-86.

2-Amino-2-deoxyglucose hydrochloride

发表于由

天然产物 糖类和糖苷 Saccharides and Glycosides

2-Amino-2-deoxyglucose hydrochloride; 纯度: ge;98.0%

2-Amino-2-deoxyglucose hydrochloride 是一种盐酸己糖胺，可用于合成环丙烯修饰的己糖胺衍生物 Ac4GlcNCyoc 和 Ac4GalNCyoc。

2-Amino-2-deoxyglucose hydrochloride

2-Amino-2-deoxyglucose hydrochloride Chemical Structure

CAS No. : 1078691-95-8

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2-Amino-2-deoxyglucose hydrochloride 相关产品

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生物活性

2-Amino-2-deoxyglucose hydrochloride is a hexosamine hydrochloride can be used in the synthesis of cyclopropene-modified hexosamine derivative Ac4GlcNCyoc and Ac4GalNCyoc[1].

分子量

215.63

Formula

C6H14ClNO5
CAS 号

1078691-95-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4deg;C, sealed storage, away from moisture

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

H2O : 125 mg/mL (579.70 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.6376 mL 23.1879 mL 46.3757 mL
5 mM 0.9275 mL 4.6376 mL 9.2751 mL
10 mM 0.4638 mL 2.3188 mL 4.6376 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Späte AK, et al. Expanding the scope of cyclopropene reporters for the detection of metabolically engineered glycoproteins by Diels-Alder reactions. Beilstein J Org Chem. 2014;10:2235-2242. Published 2014 Sep 22.

Gly6 hydrochloride(Synonyms: Hexaglycine hydrochloride)

发表于由

Gly6 hydrochloride;(Synonyms: Hexaglycine hydrochloride)

Gly6 hydrochloride (Hexaglycine hydrochloride) 是一种具有六个甘氨酸的线性甘氨酸寡肽。

Gly6 hydrochlorideamp;;(Synonyms: Hexaglycine hydrochloride)

Gly6 hydrochloride Chemical Structure

CAS No. : 71176-49-3

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生物活性

Gly6 hydrochloride (Hexaglycine hydrochloride) is a linear glycine oligopeptide with six glycines[1][2].

体外研究
(In Vitro)

The mode of action of zoocin A against sensitive streptococci is lytic, that lysis occurs as a direct result of the interaction of zoocin A with the cell, and that zoocin A and lysostaphin are both capable of cleaving the peptide substrate Gly6 (Hexaglycine)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

396.78

Formula

C12H21ClN6O7
CAS 号

71176-49-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. R S Simmonds, et al. Mode of Action of a Lysostaphin-Like Bacteriolytic Agent Produced by Streptococcus Zooepidemicus 4881. Appl Environ Microbiol. 1996 Dec;62(12):4536-41.

    [2]. S A Adibi, et al. The Number of Glycine Residues Which Limits Intact Absorption of Glycine Oligopeptides in Human Jejunum. J Clin Invest. 1977 Nov;60(5):1008-16.

Tyroserleutide hydrochloride(Synonyms: 酪丝亮肽盐酸盐)

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Tyroserleutide hydrochloride;(Synonyms: 酪丝亮肽盐酸盐) 纯度: 99.47%

Tyroserleutide hydrochloride 可从猪脾脏的降解产物中分离得到，是一种小分子三肽，在体内外均可抑制肿瘤生长。

Tyroserleutide hydrochlorideamp;;(Synonyms: 酪丝亮肽盐酸盐)

Tyroserleutide hydrochloride Chemical Structure

CAS No. : 852982-42-4

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1 mg ￥1100 In-stock
5 mg ￥2300 In-stock
10 mg ￥4000 In-stock
25 mg ￥7500 In-stock
50 mg ￥11500 In-stock
100 mg ￥19500 In-stock
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生物活性

Tyroserleutide hydrochloride, isolated from the degradation products of porcine spleen[1], is a small molecular tripeptide which inhibits tumor growth both in vitro and in vivo[2].

IC50 Target

Antitumor tripeptide[1][2]
体外研究
(In Vitro)

Tyroserleutide (YSL) exhibits immuno-modulating effects, such as enhancing concanavalin (ConA) induced proliferation of mouse spleen lymphocytes, phagocytosis of mouse peritoneal macrophages, and the activity of natural killer (NK) cells[1].
Tyroserleutide (YSL), an immunologically therapeutic tripeptide, can promote hepatocarcinoma cell (H22) apoptosis through downregulating Bcl-2 and cyclin D1 expression[2].
Tyroserleutide is an ideal choice for inducing apoptosis of liver tumor cells[2].
Tyroserleutide inhibits tumor growth and does not cause severe toxicities in the major organs. Tyroserleutide can inhibit tumor cell migration[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Tyroserleutide (10-80 μg/kg; injection (i.p.) one time every day until mice are dead) displays obvious anti-tumor activity. Tyroserleutide significantly prolongs the survival time of the murine H22 implanted mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Kun-Ming mice (18-22 g, 6 week old) with H22 tumor model[1]
Dosage: 10, 20, 40, and 80 μg/kg
Administration: Injection (i.p.) one time every day until mice were dead.
Result: Survival times are 25.53±14.14, 25.82±14.29, 30.47±17.89, 35.06±20.90 days for 10, 20, 40, and 80 μg/kg, respectively.

Clinical Trial

分子量

417.88

Formula

C18H28ClN3O6
CAS 号

852982-42-4
中文名称

酪丝亮肽盐酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:;

DMSO : 250 mg/mL (598.26 mM; Need ultrasonic)

H2O : 2 mg/mL (4.79 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3930 mL 11.9652 mL 23.9303 mL
5 mM 0.4786 mL 2.3930 mL 4.7861 mL
10 mM 0.2393 mL 1.1965 mL 2.3930 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.98 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.98 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Wang C, et al. Studies on the large scale synthesis and anti-tumor activity of YSL. Prep Biochem Biotechnol. 2003 Aug;33(3):189-95.

    [2]. Liang P, et al. pH-Triggered Conformational Change of Antp-Based Drug Delivery Platform for Tumor Treatment with Combined Photothermal Therapy and Chemotherapy. Adv Healthc Mater. 2019 Aug;8(15):e1900306.

BH3 hydrochloride

发表于由

BH3 hydrochloride;

BH3 hydrochloride 是能透过血脑屏障的多肽，通过直接激活促凋亡 Bax/Bak 或通过中和抗凋亡 Bcl-2 蛋白 (Bcl-2、Bcl-XL、Bcl-w、mcl1和A-1)来诱导细胞凋亡，通过与BH3 结构域结合。

BH3 hydrochlorideamp;;

BH3 hydrochloride Chemical Structure

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生物活性

BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian[1][2].

分子量

2677.45

Formula

C120H183ClN36O32
Sequence

Ile-Trp-Ile-Ala-Gln-Glu-Leu-Arg-Arg-Ile-Gly-Asp-Glu-Phe-Asn-Ala-Tyr-Tyr-Ala-Arg-Arg
Sequence Shortening

IWIAQELRRIGDEFNAYYARR
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Guang Yang, et al. Modulating Protein-Protein Interactions In Vivo via Peptide-Lanthanide-Derived Nanoparticles for Hazard-Free Cancer Therapy. J Biomed Nanotechnol. 2019 Sep 1;15(9):1937-1947.

    [2]. Shatrunajay Shukla, et al. BH3-only Protein BIM: An Emerging Target in Chemotherapy. Eur J Cell Biol. 2017 Dec;96(8):728-738.

Glucagon (1-29), bovine, human, porcine hydrochloride(Synonyms: 盐酸胰高血糖素 Porcine glucagon hydrochloride)

发表于由

Glucagon (1-29), bovine, human, porcine hydrochloride;(Synonyms: 盐酸胰高血糖素; Porcine glucagon hydrochloride)

Glucagon (1-29), bovine, human, porcine hydrochloride 是由胰腺 α 细胞产生的一种多肽激素。Glucagon (1-29), bovine, human, porcine hydrochloride 促进糖异生。Glucagon (1-29), bovine, human, porcine hydrochloride 可激活 HNF4α 并促进 HNF4α 磷酸化。

Glucagon (1-29), bovine, human, porcine hydrochlorideamp;;(Synonyms: 盐酸胰高血糖素; Porcine glucagon hydrochloride)

Glucagon (1-29), bovine, human, porcine hydrochloride Chemical Structure

CAS No. : 28270-04-4

规格 是否有货
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生物活性

Glucagon (1-29), bovine, human, porcine hydrochloride is a peptide hormone, produced by pancreatic α-cells. Glucagon hydrochloride stimulates gluconeogenesis[1]. Glucagon (1-29), bovine, human, porcine hydrochloride activates HNF4α and increases HNF4α phosphorylation[2][3].

体外研究
(In Vitro)

Upon binding to its receptor Gcgr, Glucagon activates cAMP-PKA signaling to stimulate hepatic glucose production (HGP) and cause hyperglycemia[1].
Glucagon stimulates both hepatic kisspeptin1 production and gluconeogenesis[1].
Glucagon (100 nM) represses CYP7A1 mRNA expression in human primary hepatocytes[3].
Glucagon (100 nM) increases phosphorylayion of HNF4α[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

Cell Line: Human primary hepatocytes (H1211, HH1215)
Concentration: 100 nM
Incubation Time:
Result: Resulted in a marked increase in the amount of phosphorylated HNF4α.

体内研究
(In Vivo)

Low-dose (20 μg/kg) Glucagon increases glycemia and does not stimulate insulin secretion in ambient-fed mice. High-dose (1 mg/kg) Glucagon lowers glycemia compared with PBS control and stimulates insulin secretion in ambient-fed mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (12- to 24-week-old)[4]
Dosage: 20 μg/kg and 1 mg/kg
Administration: Administered by i.p. injection; 45 minutes
Result: Low-dose (20 μg/kg) increased glycemia and did not stimulate insulin secretion.
High-dose (1 mg/kg) lowered glycemia and stimulated insulin secretion.

分子量

3519.21

Formula

ClH
CAS 号

28270-04-4
Sequence

His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-Leu-Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asn-Thr
Sequence Shortening

HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
中文名称

盐酸胰高血糖素
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Song WJ, et al. Glucagon regulates hepatic kisspeptin to impair insulin secretion. Cell Metab. 2014 Apr 1;19(4):667-81.

    [2]. Hirota K, et al. Hepatocyte nuclear factor-4 is a novel downstream target of insulin via FKHR as a signal-regulated transcriptional inhibitor. J Biol Chem. 2003 Apr 11;278(15):13056-60.

    [3]. Song KH, et al. Glucagon and cAMP inhibit cholesterol 7alpha-hydroxylase (CYP7A1) gene expression in humanhepatocytes: discordant regulation of bile acid synthesis and gluconeogenesis. Hepatology. 2006 Jan;43(1):117-25.

    [4]. Capozzi ME, et al. Glucagon lowers glycemia when β-cells are active. JCI Insight. 2019 Jul 23;5. pii: 129954.

A-30912A nucleus hydrochloride

发表于由

A-30912A nucleus hydrochloride;

A-30912A nucleus hydrochloride 是 Echinocandin B (ECB) 脱酰酶催化反应的产物。

A-30912A nucleus hydrochlorideamp;;

A-30912A nucleus hydrochloride Chemical Structure

CAS No. : 1029890-89-8

规格 是否有货
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生物活性

A-30912A nucleus hydrochloride is the product of the reaction catalyzed by Echinocandin B (ECB) deacylase[1].

体外研究
(In Vitro)

Echinocandin B (ECB), obtained by the fermentation of Aspergillus nidulans and Aspergillus rugulosus, is known as one of the natural cyclic hexapeptides that have a linoleoyl side chain, which inhibits a crucial enzyme in fungal cell wall biosynthesis, β-(1,3)-D-glucan synthase[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

834.27

Formula

C34H52ClN7O15
CAS 号

1029890-89-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lei Shao, et al. Efficient bioconversion of echinocandin B to its nucleus by overexpression of deacylase genes in different host strains. Appl Environ Microbiol. 2013 Feb;79(4):1126-33.

HAIYPRH hydrochloride

发表于由

HAIYPRH hydrochloride;

HAIYPRH hydrochlorid，一种靶向配体，能与转铁蛋白受体 (TfR) 特异结合。HAIYPRH hydrochlorid 可介导纳米载体通过血脑屏障的转运。

HAIYPRH hydrochlorideamp;;

HAIYPRH hydrochloride Chemical Structure

规格 是否有货
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生物活性

HAIYPRH hydrochloride, a targeting ligand, can specially bind to transferrin receptor (TfR). HAIYPRH hydrochloride can mediate the transport of nanocarriers across the blood-brain barrier[1].

体外研究
(In Vitro)

HAIYPRH hydrochloride (T7) is conjugated to liposomes for ischemic stroke targeting treatment of a novel neuroprotectant (HY-100456: ZL006)[2].
HAIYPRH hydrochloride is a heptapeptide that can be used to target gliomas[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

HAIYPRH hydrochloride, a transferrin receptor-specific peptide, is chosen as the ligand to target the co-delivery system to the tumor cells expressing transferrin receptors. HAIYPRH-modified co-delivery system shows higher efficiency in cellular uptake and gene expression than unmodified co-delivery system in U87 MG cells, and accumulated in tumor more efficiently in vivo[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

929.46

Formula

C41H61ClN14O9
Sequence Shortening

HAIYPRH
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Liu S, et al. Gene and doxorubicin co-delivery system for targeting therapy of glioma. Biomaterials. 2012;33(19):4907‐4916.

    [2]. Wang Z, et al. Enhanced anti-ischemic stroke of ZL006 by T7-conjugated PEGylated liposomes drug delivery system. Sci Rep. 2015;5:12651. Published 2015 Jul 29.

    [3]. Ziyang Zhu, et al. Goat milk-derived exosomes Endowed with Radioactive and Targeting Properties: potential to provide PET/CT monitoring for exosomes-based drug delivery system in gliomas therapy. J Nucl Med May 1, 2020 vol. 61.

His-Pro hydrochloride

发表于由

His-Pro hydrochloride;

His-Pro hydrochloride 是一种由组氨酰和脯氨酸组成的二肽。

His-Pro hydrochlorideamp;;

His-Pro hydrochloride Chemical Structure

规格 价格 是否有货
10 mg ￥950 询问价格 货期

* Please select Quantity before adding items.

生物活性

His-Pro hydrochloride is a dipeptide consisting of histidyl and proline.

分子量

288.73

Formula

C11H17ClN4O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Park SW, et al. Alterations in pancreatic protein expression in STZ-induced diabetic rats and genetically diabetic mice in response to treatment with hypoglycemic dipeptide Cyclo (His-Pro). Cell Physiol Biochem. 2012;29(3-4):603-16.

Doxorubicin hydrochloride(Synonyms: 盐酸阿霉素; Hydroxydaunorubicin hydrochloride)

发表于由

天然产物醌类Quinones

Doxorubicin hydrochloride (Synonyms: 盐酸阿霉素; Hydroxydaunorubicin hydrochloride) 纯度: 98.44%

Doxorubicin (Hydroxydaunorubicin) hydrochloride是一种具有细胞毒性的蒽环类抗生素，是一种抗癌化疗试剂。Doxorubicin hydrochloride 是一种有效的人类 DNA topoisomerase I 和 topoisomerase II 抑制剂，IC50 分别为 0.8 μM 和 2.67 μM。Doxorubicin hydrochloride 可降低 AMPK 及其下游靶蛋白乙酰辅酶 A 羧化酶的磷酸化。还可诱导凋亡 (apoptosis) 和自噬。

Doxorubicin hydrochloride(Synonyms: 盐酸阿霉素; Hydroxydaunorubicin hydrochloride)

Doxorubicin hydrochloride Chemical Structure

CAS No. : 25316-40-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥990 In-stock
50 mg ￥900 In-stock
100 mg ￥1600 In-stock
200 mg ￥3000 In-stock
500 mg ￥5000 In-stock
1 g ￥8500 In-stock
5 g   询价  
10 g   询价  

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生物活性

Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy[1][2][3].

IC50 & Target[1][2][3]

Topoisomerase II

2.67 μM (IC50)

Daunorubicins/Doxorubicins

 

Topoisomerase I

0.8 μM (IC50)

HIV-1

 

体外研究
(In Vitro)

Doxorubicin hydrochloride (1-8 µM; 24 and 48 hours) decreases the viability of MCF-10F, MCF-7 and MDA-MB-231 cells in a time- and dose-dependent manner[4].
Doxorubicin hydrochloride (1 μM; 3 and 24 hours) results in Hct-116 human colon carcinoma cells reduction in G0/G1 phase and accumulation in G2 phase[5].
Doxorubicin hydrochloride (1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells; 48 hours) induces apoptosis by upregulating Bax, caspase-8 and caspase-3 and downregulation of Bcl-2 protein expression[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

Cell Line: Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration: 0, 1, 2, 4 and 8 μM
Incubation Time: 24 and 48 hours
Result: IC50 was 1 μM for both MCF-10F and MDA-MB-231 cell lines.
IC50 was 4 μM for MCF-7 cell line.

Cell Cycle Analysis[5]

Cell Line: Hct-116 human colon carcinoma cells
Concentration: 1 μM
Incubation Time: 3 hours and 24 hours
Result: Both, bolus (3 h) and continuous (24 h) incubation led to a significant reduction of cells in G0/G1 and accumulation in G2 phase.

Western Blot Analysis[4]

Cell Line: Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration: 1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells
Incubation Time: 48 hours
Result: Bax protein expression was upregulated in MCF-10F and MDA-MB-231 cell lines but MCF-7 cells did not show any significant increase.
Caspase-8 gene expression was upregulated in MCF-10F, but it was downregulated in MCF-7 and MDA-MB-231 cells.

体内研究
(In Vivo)

Treatment with Doxorubicin (2 mg/kg) or Zoledronic acid (100 μg/kg) alone does not statistically significantly decrease final tumor volume compared with saline. Mice treated with Doxorubicin plus Zoledronic acid have statistically significantly smaller final tumor volumes than those treated with Doxorubicin alone[6].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female MF1 nu/nu mice bearing MDA-G8 breast tumor xenograft (6-week-old)[6]
Dosage: Doxorubicin (2 mg/kg); Zoledronic acid (100 μg/kg)
Administration: Intravenous injection; once a week; 6 weeks
Result: Moderate inhibition of subcutaneous tumor growth in mice that were treated with 2 mg/kg Doxorubicin alone or with 100 μg/kg Zoledronic acid alone compared to the saline control.
Mice treated with Zoledronic acid and Doxorubicin together had statistically significant smaller mean tumor volumes on day 42 than those treated with Doxorubicin alone.

Clinical Trial

分子量

579.98

Formula

C27H30ClNO11
CAS 号

25316-40-9
中文名称

盐酸阿霉素；盐酸多柔比星
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 35.71 mg/mL (61.57 mM; ultrasonic and warming and heat to 60°C)

H2O : 20 mg/mL (34.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7242 mL 8.6210 mL 17.2420 mL
5 mM 0.3448 mL 1.7242 mL 3.4484 mL
10 mM 0.1724 mL 0.8621 mL 1.7242 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.75 mg/mL (4.74 mM); Clear solution

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.59 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. John L. Nitiss, et al. Targeting DNA topoisomerase II in cancer chemotherapy.Nat Rev Cancer. 2009 May;9(5):338-50.

    [2]. Hee-KyungRhee,et al. Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones. Bioorg Med Chem. 2007 Feb 15;15(4):1651-8.

    [3]. P D Foglesong, et al. Doxorubicin inhibits human DNA topoisomerase I. Cancer Chemother Pharmacol. 1992;30(2):123-5.

    [4]. Nesstor Pilco-Ferreto, et al. Influence of doxorubicin on apoptosis and oxidative stress in breast cancer cell lines. Int J Oncol. 2016 Aug;49(2):753-62.

    [5]. Regine Lüpertz, et al. Dose- and time-dependent effects of doxorubicin on cytotoxicity, cell cycle and apoptotic cell death in human colon cancer cells. Toxicology. 2010 May 27;271(3):115-21.

    [6]. Penelope D Ottewell, et al. Antitumor effects of doxorubicin followed by zoledronic acid in a mouse model of breast cancer. J Natl Cancer Inst. 2008 Aug 20;100(16):1167-78.