产品
编 号：F095982
分子式：C22H22N4O7
分子量：454.43
分子式：C22H22N4O7
分子量：454.43
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1253584-84-7
产品详情
生物活性：
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
体内研究：
NMS-E973 (60 mg/kg; i.v.) inhibits the growth of A375 tumors subcutaneously or intracranially implanted in mice. NMS-E973 exhibits moderate elimination half-lives (5.55±1.07 h) due to high plasma clearance (39.9±1.70 mL/min/kg) combined with large volumes of distribution (5.83±3.18 L/kg) following intravenous administration (10 mg/kg) in mice.Animal Model:Balb/c male nude mice (aged 6 to 8 weeks) xenografted with the A375 tumors
Dosage:60 mg/kg
Administration:Administered twice daily i.v. according to 2 schedules: (i) every other day for 12 days and (ii) 3 days on/1 day off/3 days on (3-1-3, one cycle).
Result:Both schedules resulted in tumor shrinkage and TGI of 74% and 89%, respectively.
体外研究：
NMS-E973 inhibits cancer cell proliferation. NMS-E973 shows a widespread antiproliferative activity, with an average IC50 of 1.6 μM and 15 cell lines with an IC50 NMS-E973 相关抗体:Cell Proliferation AssayCell Line:Carcinoma breast DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells; Leukemia MV-4-11 and MOLM-13 cells; Melanoma A-375 cells
Concentration:
Incubation Time:24, 48, 72 hours
Result:IC50s of 13, 16, 56, 61, 73, 76, and 89 nM for DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells, respectively.IC50s of 29 and 35 nM for MV-4-11, MOLM-13 cells, respectively.The IC50 of 133 nM for A-375 cell.
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
体内研究：
NMS-E973 (60 mg/kg; i.v.) inhibits the growth of A375 tumors subcutaneously or intracranially implanted in mice. NMS-E973 exhibits moderate elimination half-lives (5.55±1.07 h) due to high plasma clearance (39.9±1.70 mL/min/kg) combined with large volumes of distribution (5.83±3.18 L/kg) following intravenous administration (10 mg/kg) in mice.Animal Model:Balb/c male nude mice (aged 6 to 8 weeks) xenografted with the A375 tumors
Dosage:60 mg/kg
Administration:Administered twice daily i.v. according to 2 schedules: (i) every other day for 12 days and (ii) 3 days on/1 day off/3 days on (3-1-3, one cycle).
Result:Both schedules resulted in tumor shrinkage and TGI of 74% and 89%, respectively.
体外研究：
NMS-E973 inhibits cancer cell proliferation. NMS-E973 shows a widespread antiproliferative activity, with an average IC50 of 1.6 μM and 15 cell lines with an IC50 NMS-E973 相关抗体:Cell Proliferation AssayCell Line:Carcinoma breast DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells; Leukemia MV-4-11 and MOLM-13 cells; Melanoma A-375 cells
Concentration:
Incubation Time:24, 48, 72 hours
Result:IC50s of 13, 16, 56, 61, 73, 76, and 89 nM for DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells, respectively.IC50s of 29 and 35 nM for MV-4-11, MOLM-13 cells, respectively.The IC50 of 133 nM for A-375 cell.
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