A-1331852|1430844-80-6|-陌孚医药/Medlife

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A-1331852

目录号: PL04936 纯度: ≥99%

CAS No. :1430844-80-6

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中文名称	A-1331852
中文别名	BCL-XL抑制剂(A-1331852);化合物A1331852;3-(1-(金刚烷-1-基甲基)-5-甲基-1H-吡唑-4-基)-6-(8-(苯并[D]噻唑-2-基氨基甲酰基)-3,4-二氢异喹啉-2(1H)-基)吡啶-2-酸
英文名称	A-1331852
英文别名	A-1331852;A 1331852;3-[1-(1-adamantylmethyl)-5-methylpyrazol-4-yl]-6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]pyridine-2-carboxylic acid;GTPL11102;BCP18310;BDBM50162797;s7801;A1331852;3-(1-(((3r,5r,7r)-adamantan-1-yl)methyl)-5-methyl-1H-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)picolinic acid;3-(1-(adamantan-1-ylmethyl)-5-methyl-1H-pyrazol-4-yl)-6;CID 71565985
Cas No.	1430844-80-6
分子式	C₃₈H₃₈N₆O₃S
分子量	658.81
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	A-1331852是具有口服活性的BCL-XL选择性抑制剂，K_i值小于10 pM。
生物活性	A-1331852 is an orally available BCL-XL selective inhibitor with a K i of less than 10 pM.
性状	Solid
IC50 & Target[1][2]	Bcl-xL 0.01 nM (Ki) Bcl-W 4 nM (Ki)
体外研究(In Vitro)	A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells with IC50s in the low nanomolar range but does not affect MEF cells lacking BAK or BAX. In CellTiter-Glo cell viability assay, A-1331852 inhibits NCI-H847, NCI-H1417, SET-2, HEL, OCI-M2 with EC50 values of 3, 7, 80, 120 and 100 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent. Additionally, A-1331852 combines with venetoclax to recapitulate the efficacy of navitoclax in the NCI-H1963.FP5 xenograft model of SCLC. A-1331852 significantly inhibits tumor growth in seven subcutaneous xenograft models of solid tumors, including breast cancer, NSCLC, and ovarian cancer. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279ra40.

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (75.89 mM)Ethanol : 4 mg/mL (6.07 mM; ultrasonic and warming and heat to 60°C)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)

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