ETP-46321 |CAS:1252594-99-2 Probechem Biochemicals

Chemical Structure : ETP-46321

CAS No.: 1252594-99-2

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ETP-46321 (ETP 46321;ETP46321)

货号: PC-42989Not For Human Use, Lab Use Only.

ETP-46321 is a potent, selective, orally bioavailable dual PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM, weakly inhibits p110β and p110γ with IC50 of 170 and 179 nM.

规格	价格	库存
5 mg	￥2180	In stock
10 mg	￥3680	In stock
25 mg	￥5280	In stock
100 mg		Get quote

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生物&药学活性

ETP-46321 is a potent, selective, orally bioavailable dual PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM, weakly inhibits p110β and p110γ with IC50 of 170 and 179 nM.
ETP-46321 shows highly selectivity versus mTOR and 288 representative kinases, also potently inhibits mutants PI3K α E542K, E545K, and H1047R with IC50 of ~2 nM.
ETP-46321 inhibits phosphorylation of AKT Ser473 in the U2OS cell line with IC50 of 8.3 nM.
ETP-46321 shows significant tumor growth inhibition and reduction of the tumor metabolic activity in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation.

物理化学性质&存储条件

分子量	473.5519
分子式	C20H27N9O3S
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	DMSO: ≥ 33 mg/mL
Chemical Name/SMILES	2-Pyrimidinamine, 5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]-

参考文献

1. Martínez González S, et al. Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6.

2. Granda TG, et al. Invest New Drugs. 2013 Feb;31(1):66-76.

3. Aragoneses-Fenoll L, et al. Biochem Pharmacol. 2016 Apr 15;106:56-69.

ETP-46321 (ETP 46321;ETP46321)

生物&药学活性

物理化学性质&存储条件

参考文献

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ETP-46321 (ETP 46321;ETP46321)

生物&药学活性

物理化学性质&存储条件

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