G12Si-5 | K-Ras(G12S) inhibitor | Probechem Biochemicals

Chemical Structure : G12Si-5

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G12Si-5 (K-Ras(G12S) inhibitor)

货号: PC-49153Not For Human Use, Lab Use Only.

G12Si-5 is a specific small molecule that covalently targets K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

G12Si-5 is a specific small molecule that covalently targets K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.
G12Si-5 inhibits Ras signaling in A549 cells with IC50 of 3 uM, does not perturb the signaling in A375 cells (wild-type KRAS) or SW1990 cells (homozygous KRAS p.G12D).
G12Si-5 dose-dependently reduces phospho-ERK levels in Ba/F3:K-Ras(G12S) cells, also inhibits the growth of KMS20, a patient-derived myeloma cell line with a homozygous KRAS p.G12S mutation, with IC50 of 7.5 uM.

物理化学性质&存储条件

分子量	574.053
分子式	C31H29ClFN5O3
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	(1R,6R)-3-(7-(8-chloronaphthalen-1-yl)-8-fluoro-2-((tetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)pyrido[4,3-d]pyrimidin-4-yl)-8-oxa-3-azabicyclo[4.2.0]octan-7-one

参考文献

1. Ziyang Zhang, et al. Nat Chem Biol. 2022 Jul 21. doi: 10.1038/s41589-022-01065-9.