1253584-84-7
1253584-84-7 structure
- Name: NMS-E973
- Chemical Name: nms-e973
- CAS Number: 1253584-84-7
- Molecular Formula: C22H22N4O7
- Molecular Weight: 454.43300
- Catalog: Biochemical Inhibitor Cytoskeletal Signaling HSP eg HSP90 inhibitor
- Create Date: 2017-08-09 12:10:24
- Modify Date: 2024-01-31 19:03:23
-
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[1].
| Name | nms-e973 |
|---|
| Description | 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[1]. |
|---|---|
| Related Catalog | |
| Target |
HSP90α:10 nM (DC50) |
| In Vitro | 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 <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 IC50 of 133 nM for A-375 cell. |
| 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. |
| References |
| Molecular Formula | C22H22N4O7 |
|---|---|
| Molecular Weight | 454.43300 |
| Exact Mass | 454.14900 |
| PSA | 153.88000 |
| LogP | 4.12930 |
| Storage condition | -20℃ |