NMS-E973 是一种有效的，可透过血脑屏障的选择性HSP90抑制剂。NMS-E973 与Hsp90α的 ATP 位点结合，DC50小于 10 nM。NMS-E973 能够穿越血脑屏障 (BBB)。具有抗肿瘤效果。
| 生物活性 | NMS-E973 is a potent and selective inhibitor ofHSP90. NMS-E973 binds to the ATP binding site ofHsp90αwith aDC50of<10 nm. nms-e973 is able to cross the blood-brain barrier (bbb). antitumor efficacy[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | NMS-E973 inhibits cancer cell proliferation. NMS-E973 shows a widespread antiproliferative activity, with an average IC50of 1.6 μM and 15 cell lines with an IC50<100 nm[1].
Cell Proliferation Assay[1] | Cell 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 IC50of 133 nM for A-375 cell. |
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体内研究
(In Vivo) | NMS-E973 (60 mg/kg; i.v.) inhibits the growth of A375 tumors subcutaneously or intracranially implanted in mice[1].
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[1].
| Animal Model: | Balb/c male nude mice (aged 6 to 8 weeks) xenografted with the A375 tumors[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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