An inhibitor of Plk1 (IC50 = 2 nM); selective for Plk1 over Plk2 and Plk3 (IC50s = >10

NMS-1286937 – 5 mg

Brand:
Cayman
CAS:
1034616-18-6
Storage:
-20
UN-No:
Non-Hazardous - /

NMS-1286937 is an inhibitor of polo-like kinase 1 (Plk1; IC50 = 2 nM).{20485} It is selective for Plk1 over Plk2 and Plk3 (IC50s = >10,000 nM for both). It inhibits proliferation of A2780 cells with an IC50 value of 42 nM. NMS-1286937 halts the cell cycle at the G2/M phase in A2780 cells when used at a concentrations ranging from 20 to 200 nmol/L and induces apoptosis.{52131} It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 60 mg/kg once per day.{20485} NMS-1286937 (45 mg/kg) also induces tumor regression in an HT-29 mouse xenograft model when administered in combination with CPT11 (irinotecan; Item No. 14180).{52131}  

 

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Description

An inhibitor of Plk1 (IC50 = 2 nM); selective for Plk1 over Plk2 and Plk3 (IC50s = >10,000 nM for both); inhibits proliferation of A2780 cells (IC50 = 42 nM); halts the cell cycle at the G2/M phase in A2780 cells at 20-200 nmol/L and induces apoptosis; reduces tumor growth in an HCT116 mouse xenograft model at 60 mg/kg once per day; induces tumor regression in an HT-29 mouse xenograft model at 45 mg/kg in combination with CPT11

Formal name: 4,5-dihydro-1-(2-hydroxyethyl)-8-[[5-(4-methyl-1-piperazinyl)-2-(trifluoromethoxy)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

Synonyms:  NMS-P937|Onvansertib|PCM-075

Molecular weight: 532.5

CAS: 1034616-18-6

Purity: ≥98%

Formulation: A solid

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