产品
编 号：F147761
分子式：C50H57ClN8O7S3
分子量：1013.69
分子式：C50H57ClN8O7S3
分子量：1013.69
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CAS No: 1391108-10-3
产品详情
生物活性：
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM.
体内研究：
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.BM-1074 (i.v., 15 mg/kg, single) induces strong apoptosis in H146 tumor tissues.Animal Model:SCID mice (injected with 5 x 106 H146 cancer cells with Matrigel,subcutaneously)
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 106 H146 cancer cells with Matrigel,subcutaneously)
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.
体外研究：
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.
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM.
体内研究：
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.BM-1074 (i.v., 15 mg/kg, single) induces strong apoptosis in H146 tumor tissues.Animal Model:SCID mice (injected with 5 x 106 H146 cancer cells with Matrigel,subcutaneously)
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 106 H146 cancer cells with Matrigel,subcutaneously)
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.
体外研究：
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.
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