Dolastatin 15(Synonyms: DLS 15)

Dolastatin 15;(Synonyms: DLS 15)

Dolastatin 15 (DLS 15),一种从 Dolabella auricularia 中提取的去甲肽,是一种有效的抗有丝分裂剂 (antimitotic),在结构上与抗微管蛋白剂 Dolastatin 10 有关。Dolastatin 15 诱导多发性骨髓瘤细胞周期阻滞和凋亡。Dolastatin 15 可作为 ADC 细胞毒素。

Dolastatin 15amp;;(Synonyms: DLS 15)

Dolastatin 15 Chemical Structure

CAS No. : 123884-00-4

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生物活性

Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin[1][2][3].

IC50 Target

Auristatin

;

体外研究
(In Vitro)

Dolastatin 15 (DLS 15) induces cell cycle arrest at the G2/M phase followed by apoptosis in various human myeloma cell lines (RPMI8226, U266, and IM9). Dolastatin 15 induces apoptosis of myeloma cells via activation of both mitochondrial- and Fas (CD95)/Fas-L (CD95-L)-mediated pathways[2]. Dolastatin 15 (DLS 15) displays growth inhibitory activity against all four SCLC cell lines (NCI-H69, NCI-H82, NCI-H345, NCI-H446) with IC50 values ranging from 0.039-28.8 nM, which were 2.7-9.2-fold higher than the values for dolastatin 10. All four SCLC cell lines underwent G2/M arrest within 24 hours of exposure to dolastatin 15[4].

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

体内研究
(In Vivo)

Dolastatin 15 conjugates to Trastuzumab via lysine residues at the drug C-terminus using a non-cleavable linker (Trastuzumab-amide-C-term-Dol15) produced target-dependent growth inhibition of cells endogenously expressing high HER2 levels (i.e., SK-BR-3, SK-OV-3) in vitro. This ADC was effective at varying doses (i.e., 10 and 20 mg/kg) in the SK-OV-3 human ovarian cancer xenograft[3].

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

分子量

837.06

Formula

C45H68N6O9

CAS 号

123884-00-4

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]. Bai R, et al. Dolastatin 15, a potent antimitotic depsipeptide derived from Dolabella auricularia. Interaction with tubulin and effects of cellular microtubules. Biochem Pharmacol. 1992 Jun 23;43(12):2637-45.

    [2]. Sato M, et al. A natural peptide, dolastatin 15, induces G2/M cell cycle arrest and apoptosis of human multiple myeloma cells. Int J Oncol. 2007 Jun;30(6):1453-9.

    [3]. Gianolio DA, et al. Targeting HER2-positive cancer with dolastatin 15 derivatives conjugated to trastuzumab, novel antibody-drug conjugates. Cancer Chemother Pharmacol. 2012 Sep;70(3):439-49.

    [4]. Ali MA, et al. Dolastatin 15 induces apoptosis and BCL-2 phosphorylation in small cell lung cancer cell lines. Anticancer Res. 1998 Mar-Apr;18(2A):1021-6.

Dolastatin 10(Synonyms: DLS 10 NSC 376128)

Dolastatin 10;(Synonyms: DLS 10; NSC 376128) 纯度: 98.63%

Dolastatin 10 (DLS 10) 是一种有效的抗有丝分裂肽,抑制微管蛋白聚合。

Dolastatin 10amp;;(Synonyms: DLS 10;  NSC 376128)

Dolastatin 10 Chemical Structure

CAS No. : 110417-88-4

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1 mg ¥3000 In-stock
5 mg ¥8000 In-stock
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Dolastatin 10 相关产品

bull;相关化合物库:

  • Natural Product Library Plus
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  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library
  • Peptide Library

生物活性

Dolastatin 10 (DLS 10) is a potent antimitotic peptide that inhibits tubulin polymerization.

IC50 Target

Auristatin

;

体外研究
(In Vitro)

Dolastatin 10 is a unique pentapeptide that isolated from the sea hare Dolabella auricularia. These in vitro data are quite comparable to those of Dolastatin 10 and Auristatin PE, each of which has GI50 values of 10−5-10−6 μg/mL (10−2-10−3 nM) against a similar minipanel of human cell lines[2]. The antibody-drug conjugate (ADC) comprises the anti-CD30 monoclonal antibody cAC10 conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), a synthetic analog of the tubulin polymerization inhibitor Dolastatin 10[3].

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

Clinical Trial

分子量

785.09

Formula

C42H68N6O6S

CAS 号

110417-88-4

中文名称

尾海兔素10

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
In Vitro:;

DMSO : ≥ 100 mg/mL (127.37 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2737 mL 6.3687 mL 12.7374 mL
5 mM 0.2547 mL 1.2737 mL 2.5475 mL
10 mM 0.1274 mL 0.6369 mL 1.2737 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

参考文献
  • [1]. Pitot HC, et al. Phase I trial of dolastatin-10 (NSC 376128) in patients with advanced solid tumors. Clin Cancer Res. 1999 Mar;5(3):525-31.

    [2]. Pettit GR, et al. Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications ofdolastatin 10. J Nat Prod. 2011 May 27;74(5):962-8.

    [3]. Brentuximab vedotin. Drugs R D. 2011;11(1):85-95.