KRAS inhibitor-9

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KRAS inhibitor-9

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

300809-71-6

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

KRASinhibitor-9是有效的KRAS抑制剂(Kd=92μM)，阻止GTP-KRAS的形成和KRAS下游激活。KRASinhibitor-9以中等的结合亲和力与KRASG12D，KRASG12C和KRASQ61H蛋白结合。KRASinhibitor-9导致G2/M细胞周期停滞并诱导凋亡(apoptosis)。KRASinhibitor-9选择性抑制具有KRAS突变的NSCLC细胞的增殖，但不抑制正常肺细胞的增殖。KRASinhibitor-9

Cas No.	300809-71-6
别名	4-(苯并[D]噻唑-2-基硫基)-3-氯苯胺
Canonical SMILES	NC1=CC=C(SC2=NC3=CC=CC=C3S2)C(Cl)=C1
分子式	C₁₃H₉ClN₂S₂
分子量	292.81
溶解度	DMSO: 250 mg/mL (853.80 mM)
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells[1]. KRAS inhibitor-9 bound to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity of -5.38, -5.41, and -3.97 kcal/mol, respectively[1]. KRAS inhibitor-9 (0-100 μM) shows strong inhibition selectivity in NSCLC cells with IC50s ranging from 39.56 to 66.02 μM for H2122, H358 and H460 cells (at 72 hours)[1].KRAS inhibitor-9 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells[1].KRAS inhibitor-9 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway[1].KRAS inhibitor-9 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC[1]. Cell Viability Assay[1] Cell Line: H2122 (KRAS G12C), H358 (KRAS G12C) and H460 (KRAS Q61H) cell lines [1]. Xie C, et al. Identification of a New Potent Inhibitor Targeting KRAS in Non-small Cell Lung Cancer Cells. Front Pharmacol. 2017;8:823. Published 2017 Nov 14.