| Identification | Back Directory | [Name]
Spiro[5,7-etheno-1H,11H-cyclobut[i][1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-2(3H),1'(2'H)-naphthalen]-8(9H)-one, 6'-chloro-3',4',12,13,16,16a,17,18,18a,19-decahydro-16-methoxy-11,12-dimethyl-16-[[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl]-, 10,10-dioxide, (1'S,11R,12S,14E,16R,1... | [CAS]
2245848-05-7 | [Synonyms]
AMG 397
Murizatoclax
Spiro[5,7-etheno-1H,11H-cyclobut[i][1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-2(3H),1'(2'H)-naphthalen]-8(9H)-one, 6'-chloro-3',4',12,13,16,16a,17,18,18a,19-decahydro-16-methoxy-11,12-dimethyl-16-[[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl]-, 10,10-dioxide, (1'S,11R,12S,14E,16R,1... | [Molecular Formula]
C42H57ClN4O5S | [MDL Number]
MFCD34470082 | [MOL File]
2245848-05-7.mol | [Molecular Weight]
765.44 |
| Hazard Information | Back Directory | [Uses]
Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer[1][2]. | [in vivo]
Murizatoclax (25-50 mg/kg; p.o. once or twice weekly) exhibits significant tumor regressions in mice bearing OPM2 xenografts[2].
Murizatoclax (10-60 mg/kg; p.o. twice weekly) achieves 47% MOLM-13 orthotopic tumor growth inhibition (TGI), 99% TGI and 75% regression at the dose of 10, 30 and 60 mg/kg, respectively[2]. | [IC 50]
MCL1: 15 pM (Ki) | [References]
[1] Wang H, et, al. Targeting MCL-1 in cancer: current status and perspectives. J Hematol Oncol. 2021 Apr 21;14(1):67. DOI:10.1186/s13045-021-01079-1
[2] Caenepeel S, et al. Abstract 6218: discovery and preclinical evaluation of AMG 397, a potent, selective and orally bioavailable MCL1 inhibitor. Cancer Res. 2020;80(16 Supplement):6218. |
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