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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-BAY-293
BAY-293

Chemical Structure : BAY-293

CAS No.: 2244904-70-7

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BAY-293 (BAY293, BAY 293)

货号: PC-36030Not For Human Use, Lab Use Only.

BAY-293 (BAY293, BAY 293) is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM.

规格 价格 库存 数量
5 mg ￥1180 In stock
10 mg ￥1880 In stock
25 mg ￥2980 In stock
50 mg ￥4880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BAY-293 (BAY293, BAY 293) is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM.
BAY-293 displays no significant activity against KRAS WT-CRAF RBD, CDC42 and EGFR (>20 uM).
BAY-293 blocks reloading of KRAS with GTP, does not stabilize KRASWT or KRASG12C.
BAY-293 inhibits the activation of RAS in HeLa cells with IC50 of 410 nM, efficiently inhibits pERK levels in K562 cells after incubation for 60 min without affecting total protein levels of ERK (IC50=180 nM).
BAY-293 shows antiproliferative activity against wild-type KRAS cell lines (K562, MOLM-13; IC50~1 uM) and cell lines with KRASG12C mutation (NCI-H358, Calu-; IC50~3 uM) by preventing formation of the KRAS-SOS1 complex, also shows synergic antiproliferative effect with covalent KRASG12C inhibitor ARS-853.
BAY-293 is a valuable chemical probe for investigation of the activation of KRAS by SOS1.

物理化学性质&存储条件

分子量 448.585
分子式 C25H28N4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-6,7-dimethoxy-2-methyl-N-(1-(4-(2-((methylamino)methyl)phenyl)thiophen-2-yl)ethyl)quinazolin-4-amine

参考文献

1. Hillig RC, et al. Proc Natl Acad Sci U S A. 2019 Jan 25. pii: 201812963. doi: 10.1073/pnas.1812963116.

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