标签归档：kras

Rineterkib

发表于由

Rineterkib; 纯度: 99.21%

Rineterkib (compound B) 是具有口服活性的 RAF 和ERK1/2 的抑制剂，通过激活 MAPK 通路中的突变来发挥抗增生作用。这种活性与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌以及 KRAS-突变型卵巢癌尤为相关。

Rineterkibamp;;

Rineterkib Chemical Structure

CAS No. : 1715025-32-3

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥2750 In-stock
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
25 mg ￥9500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Rineterkib 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Orally Active Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Rineterkib (compound B) is an orally active RAF and ERK1/2 inhibitor in the study of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1].

IC50 Target[1]

RAF

;

ERK1

;

ERK2

;

体内研究
(In Vivo)

Rineterkib (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the Calu-6 human NSCLC subcutaneous tumor xenograft model in mice[1].

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

Animal Model: Calu-6 NSCLC xenograft tumor models in mice[1].
Dosage: 50, 75 mg/kg.
Administration: Orally either daily (qd) or every other day (q2d) for 27 days.
Result: Significantly reduced the tumor volume.

分子量

578.42

Formula

C26H27BrF3N5O2
CAS 号

1715025-32-3
运输条件

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

4deg;C, sealed storage, away from moisture and light

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

DMSO : 200 mg/mL (345.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7288 mL 8.6442 mL 17.2885 mL
5 mM 0.3458 mL 1.7288 mL 3.4577 mL
10 mM 0.1729 mL 0.8644 mL 1.7288 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：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 5 mg/mL (8.64 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (8.64 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. CAPONIGRO, et al. THERAPEUTIC COMBINATIONS COMPRISING A RAF INHIBITOR AND A ERK INHIBITOR. WO2018051306A1.

SAH-SOS1A

发表于由

SAH-SOS1A;

SAH-SOS1A 是一种基于肽的 SOS1/KRAS 蛋白相互作用抑制剂。SAH-SOS1A 以纳摩尔亲和力 (EC50=106-175 nM) 与野生型和突变型 KRAS (G12D, G12V, G12C, G12S, and Q61H) 结合，直接和独立地阻断核苷酸结合，损害 KRAS 驱动的癌细胞活力，并通过阻断 KRAS 下游 ERK-MAPK 磷酸化信号级联的机制发挥作用。

SAH-SOS1Aamp;;

SAH-SOS1A Chemical Structure

CAS No. : 1652561-87-9

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

SAH-SOS1A 的其他形式现货产品:

SAH-SOS1A TFA

生物活性

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS[1].

IC50 Target[1]

KRAS-SOS1

;

KRas G12C

140 nM (EC50)

KRas G12D

109 nM (EC50)

KRas G12V

154 nM (EC50)

KRas G12S

155 nM (EC50)

KRas Q61H

175 nM (EC50)

K-Ras WT

106 nM (EC50)

体外研究
(In Vitro)

SAH-SOS1A (0.625-40 μM) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo320-HSR cells, are similarly affected[1].
SAH-SOS1A (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation[1].

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

Cell Viability Assay[1]

Cell Line: Panc 10.05 cells bearing the KRAS G12D mutation
Concentration: 0.625-40 μM
Incubation Time: 24 hours
Result: Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.

Western Blot Analysis[1]

Cell Line: Panc 10.05 cells
Concentration: 5-40 μM
Incubation Time: Indicated doses for 4 h, followed by 15-min stimulation with EGF
Result: Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.

体内研究
(In Vivo)

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85DV12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2[1].

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

2187.53

Formula

C100H159N27O28
CAS 号

1652561-87-9
Sequence Shortening

RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)
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]. Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112(6):1761-1766.

KRAS G13D peptide, 25 mer

发表于由

KRAS G13D peptide, 25 mer;

KRAS G13D peptide, 25 mer，KRAS 激活癌基因突变肽，是一种免疫增强剂。KRAS G13D peptide, 25 mer 可用于制备 KRAS 疫苗。详细信息请参考专利文献 WO2018144775A1。

KRAS G13D peptide, 25 meramp;;

KRAS G13D peptide, 25 mer Chemical Structure

CAS No. : 145019-94-9

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

KRAS G13D peptide, 25 mer, a KRAS activating oncogene mutation peptide, is an immune potentiator extracted from patent WO2018144775A1. KRAS G13D peptide, 25 mer can be used to prepare KRAS vaccine[1].

体外研究
(In Vitro)

KRAS G13D peptide, 25 mer is encoded by immunomodulatory therapeutic mRNA that can be used to prepare KRAS vaccine[1].

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

2634.10

Formula

C118H201N29O36S
CAS 号

145019-94-9
Sequence

Met-Thr-Glu-Tyr-Lys-Leu-Val-Val-Val-Gly-Ala-Gly-Asp-Val-Gly-Lys-Ser-Ala-Leu-Thr-Ile-Gln-Leu-Ile-Gln
Sequence Shortening

MTEYKLVVVGAGDVGKSALTIQLIQ
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]. Huang EYC, et, al. Immunomodulatory therapeutic mrna compositions encoding activating oncogene mutation peptides. WO2018144775A1.