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KRAS inhibitor-10

KRAS inhibitor-10

产品编号 T36761   CAS 2578876-75-0

KRAS inhibitor-10 (WO2021005165 A1, compound 11) is a potent and selective inhibitor of RAS proteins, with a specific focus on KRAS proteins. This orally active anti-cancer agent demonstrates strong efficacy in cancer research, specifically in pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS inhibitor-10 is classified as a tetrahydroisoquinoline compound. Its inhibitory properties provide valuable insights and potential therapeutic applications in the field of oncology [1].

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KRAS inhibitor-10 Chemical Structure
KRAS inhibitor-10, CAS 2578876-75-0
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 6-8周
50 mg ¥ 13,800 6-8周
100 mg ¥ 17,500 6-8周
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: KRAS inhibitor-10 (T36761)
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参考文献
产品描述 KRAS inhibitor-10 (WO2021005165 A1, compound 11) is a potent and selective inhibitor of RAS proteins, with a specific focus on KRAS proteins. This orally active anti-cancer agent demonstrates strong efficacy in cancer research, specifically in pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS inhibitor-10 is classified as a tetrahydroisoquinoline compound. Its inhibitory properties provide valuable insights and potential therapeutic applications in the field of oncology [1].
体外活性 KRAS inhibitor-10 (0.1-50 μμ; 72 hours) has antiproliferative effects in KRas mutant tumor cells, KRAS inhibitor-10 is against A549 (lung carcinoma cell line bearing KRasG12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRasG12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRasG12D oncogenic mutation) and RPMI (myeloma cell line bearing KRasG12A oncogenic mutation) cell proliferation with IC50 values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively[1].KRAS inhibitor-10 (0-1 μM, 7 days) is against cell viability in a 3D CellTiter-GloTM cell viability assay for NIH-H358 cell, the IC50 value is 0.413 μM[1].
体内活性 KRAS inhibitor-10 (oral administration; 20 mg/kg; BID; 27 days) is safe and tolerate for the bearing mice. KRAS inhibitor-10 demonstrates significant oral anti-tumor activities in vivo. And the tumor growth inhibition (TGI) value is 48.22% for KRAS inhibitor-10[1].
分子量 519.63
分子式 C30H37N3O5
CAS No. 2578876-75-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (192.44 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9244 mL 9.6222 mL 19.2445 mL 48.1112 mL
5 mM 0.3849 mL 1.9244 mL 3.8489 mL 9.6222 mL
10 mM 0.1924 mL 0.9622 mL 1.9244 mL 4.8111 mL
20 mM 0.0962 mL 0.4811 mL 0.9622 mL 2.4056 mL
50 mM 0.0385 mL 0.1924 mL 0.3849 mL 0.9622 mL
100 mM 0.0192 mL 0.0962 mL 0.1924 mL 0.4811 mL

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TargetMol Library Books参考文献

1. Miguel VEGA GARCíA, et al. Tetrahydroisoquinoline compounds. Patent wo2021002165

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

KRAS inhibitor-10 2578876-75-0 KRAS inhibitor 10 KRAS inhibitor10 Inhibitor inhibitor inhibit

 

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