產(chǎn)品目錄

規(guī)格	10 mM * 1 mL in DMSO 1mg 5mg 10mg 25mg
CAS	1799633-27-4
別名	N/A
化學(xué)名	(S)-2-(((S)-5-(3-chloro-2-methyl-4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)-6-(5-fluorofuran-2-yl)thieno[2,3-d]pyrimidin-4-yl)oxy)-3-(2-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl)methoxy)phenyl)propanoic acid
分子式	C39H37ClF4N6O6S
分子量	829.26
溶解度	≥ 41.45mg/mL in DMSO, ≥ 20mg/mL in MeOH
儲存條件	4°C, protect from light, stored under nitrogen
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

產(chǎn)品描述：

S63845 is a small molecule MCL1 inhibitor with Ki < 1.2 nM [1].

Myeloid cell leukemia 1 (MCL1) is a pro-survival protein and belongs to BCL-2 family proteins. BCL-2 family proteins are key regulators of the mitochondrial apoptotic pathway. MCL1 is overexpressed in many cancers, so inhibitors targeting this protein may kills MCL1-dependent cancer cells [1].

S63845 is a highly selective and potent MCL1 inhibitor. S63845 bound human MCL1 with KD value of 0.19 nM. S63845 was approximately 1,000-fold more potent in killing MCL1-dependent H929 multiple myeloma cells than MCL1 inhibitor A-1210477. S63845 also induced caspase-dependent phosphatidyl-serine exposure, PARP cleavage and cytochrome c release from mitochondria. In HeLa cells, S63845 disrupted binding of BAK and BAX to MCL1. S63845 killed cancer cells through activation of the BAX/BAK-dependent mitochondrial apoptotic pathway by direct inhibition of MCL1 [1].

In immunocompromised mice with human multiple myeloma (H929 and AMO1) xenografts, intravenously injected (i.v.) S63845 showed dose-dependent anti-tumour activity with maximal tumour growth inhibition (TGImax) of 103% and 114% in the H929 and AMO1 model, respectively [1].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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