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BM-1074
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BM-1074图片
CAS NO:1391108-10-3
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
BM-1074 是一种有效且特异的Bcl-2/Bcl-xL抑制剂，其IC50值分别为 1.8 nM (Bcl-2) 和 6.9 nM (Bcl-xL)，Ki值都小于 1 nM，BM-1074 可诱导细胞凋亡 (apoptosis)，对四种小细胞肺癌细胞系 (H146、H1963、H187、H1417) 有抗增殖活性，IC50值为 1-2 nM。
生物活性

BM-1074 is a potent and specificBcl-2/Bcl-xLinhibitor withKivalues of< 1 nM andIC50values of 1.8 nM and 6.9 nM forBcl-2andBcl-xL, respectively. BM-1074 inducesapoptosis, and exhibits antiproliferative activity against four small-cell lungcancercell lines (H146, H1963, H187 and H1417) withIC50values of 1-2 nM[1].

IC50& Target[1]

Bcl-2

1.8 nM (IC50)

Bcl-xL

6.9 nM (IC50)

体外研究
(In Vitro)

BM-1074 (Compound 32) shows high binding affinity to both Bcl-2 and Bcl-xL proteins and exhibits inhibitory activity against H146, H1963, H187, and H1417 cell lines[1].

Cell Proliferation Assay[1]

Cell Line:H146, H1963, H187, and H1417
Concentration:0-200 nM
Incubation Time:4 days
Result:Inhibited the cell growth of H146, H1963, H187 and H1417 cell lines with IC50values of 1.3 nM, 1.0 nM, 1.4 nM and 2.3 nM, respectively.
体内研究
(In Vivo)

BM-1074 (i.v., 15 mg/kg, daily, 5 days a week for 2 weeks) exhibits the maximum tolerated dose (MTD) (15 mg/kg) and strong antitumor activity in H146 tumor xenograft mice, as well as shows no significant weight loss (<5%) or other signs of toxicity[1].
BM-1074 (i.v., 15 mg/kg, single) induces strong apoptosis in H146 tumor tissues[1].

Animal Model:SCID mice (injected with 5 x 106H146 cancer cells with Matrigel, subcutaneously)[1]
Dosage:15 mg/kg
Administration:i.v., 15 mg/kg, daily, 5 days a week for 2 weeks
Result:Showed good toleration and did not cause significant weight loss or other signs of toxicity, also induced completely and persistent tumor regression in the H146 xenograft model.
Animal Model:SCID mice (injected with 5 x 106H146 cancer cells with Matrigel, subcutaneously)[1]
Dosage:15 mg/kg
Administration:i.v., 15 mg/kg, single dosage
Result:Induced robust cleavage of PARP and caspase-3 at both 3 and 6-hr time-points in H146 tumor tissues.
分子量

1013.69

Formula

C50H57ClN8O7S3

CAS 号

1391108-10-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.