ChemicalBook > CAS DataBase List > NMS-P937 (NMS1286937)

NMS-P937 (NMS1286937)

Product Name: NMS-P937 (NMS1286937)
CAS No.: 1034616-18-6
Chemical Name: NMS-P937 (NMS1286937)
Synonyms: PCM075;CS-1243;PCM 075;PCM-075;NMS-P937;NMS-1286937;NMS-1286937,NMS-P937;NMS-P937 (NMS1286937);Onvansertib (NMS-P937);Onvansertib（NMS-1286937
CBNumber: CB12715659
Molecular Formula: C24H27F3N8O3
Formula Weight: 532.52
MOL File: 1034616-18-6.mol

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NMS-P937 (NMS1286937) Property

Boiling point:: 757.8±70.0 °C(Predicted)
Density: 1.57±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: insoluble in H2O; insoluble in EtOH; ≥13.33 mg/mL in DMSO
form: solid
pka: 14.29±0.10(Predicted)
color: Off-white to light yellow
InChIKey: QHLVBNKYJGBCQJ-UHFFFAOYSA-N
SMILES: N1=C2C(CCC3C(C(N)=O)=NN(CCO)C=32)=CN=C1NC1=CC(N2CCN(C)CC2)=CC=C1OC(F)(F)F

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 28762
Product name: NMS-1286937
Packaging: 5mg
Price: $116
Updated: 2024/03/01

Cayman Chemical

Product number: 28762
Product name: NMS-1286937
Packaging: 25mg
Price: $381
Updated: 2024/03/01

Cayman Chemical

Product number: 28762
Product name: NMS-1286937
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 28762
Product name: NMS-1286937
Packaging: 10mg
Price: $169
Updated: 2024/03/01

TRC

Product number: N631750
Product name: NMS-P937
Packaging: 1mg
Price: $125
Updated: 2021/12/16

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NMS-P937 (NMS1286937) Chemical Properties,Usage,Production

Uses

NMS-P937 is a quinazoline derivative that is a potent and selective Polo-like kinase 1 inhibitor. Antitumor, anti-cancer.

Biological Activity

nms-1286937 (nms-p937) is a potent and selective inhibitor of polo-like kinase 1 (plk1) with ic50 value of 2 nm [1].plk1 is a serine/threonine protein kinase and plays an important role in the cell cycle control machinery. plk1 is involved in mitotic entry, bipolar mitotic spindle formation, centrosome duplication, transition from metaphase to anaphase, maintenance of genomic stability and cytokinesis [1].nms-1286937 is an orally bioavailable plk1 inhibitor. in cell lines established from solid tumors, leukemias and lymphomas, nms-p937 inhibited tumor cell proliferation. in a2780 cells, nms-p937 caused a g2-m cell-cycle block. in the mitotic phase, nms-p937 induced apoptotic death with misaligned chromosomes and an aberrant number of spindles poles [2]. in human osteosarcoma (os) cell lines, nms-p937 inhibited migration and clonogenic ability of cell lines. in abcb1-overexpressing, doxorubicin (dx)-resistant cell lines, combination of nms-p937 and dx reverted dx-resistance by inhibiting abcb1 transport activity [3].in harlan nu/nu mice, nms-p937 exhibited a good pharmacokinetic profile with low clearance, high auc and cmax, and acceptable oral bioavailability. in mice xenografted with human hct116 colon adenocarcinoma cells, nms-p937 (45 mg/kg) inhibited tumor growth by 83% and reduced body weight by 16% [1].

in vivo

NMS-1286937 (45 mg/kg, i.v.) shows a good tumor growth inhibition with acceptable and reversible body weight loss in CD1 nu/nu mice xenografted with human HCT116 colon adenocarcinoma cells. NMS-1286937 (60 mg/kg, p.o.) also inhibits the growth of tumor on HCT116 xenograft model^[1]. NMS-P937 (45 mg/kg, i.v.or 60 mg/kg, p.o) inhibits tumor growth to a comparable degree (TGI, 83% and 79% intravenously and orally, respectively) in HCT116-bearing mice. The combination of NMS-P937 (120 mg/kg given for 4 cycles of 2 consecutive days with 10-day rest) and cytarabine (75 mg/kg for 4 cycles of 5 consecutive days with 7-day rest) in the disseminated leukemia model AmL-PS is well tolerated and clearly showed increased mice survival^[2]. NMS-P937 (60 mg/kg bid os per day over 2 days with a 5 day rest) shows good efficacy compared to standard therapies, with a significant increase in median survival time (MST) in the established disease setting^[3].

IC 50

PLK1: 2 nM (IC₅₀); FLT3: 510 nM (IC₅₀); MELK: 744 nM (IC₅₀); CK2: 826 nM (IC₅₀)

References

[1]. beria i, bossi rt, brasca mg, et al. nms-p937, a 4,5-dihydro-1h-pyrazolo[4,3-h]quinazoline derivative as potent and selective polo-like kinase 1 inhibitor. bioorg med chem lett, 2011, 21(10): 2969-2974.
[2]. valsasina b, beria i, alli c, et al. nms-p937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. mol cancer ther, 2012, 11(4): 1006-1016.
[3]. sero v, tavanti e, vella s, et al. targeting polo-like kinase 1 by nms-p937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance. invest new drugs, 2014, 32(6): 1167-1180.

NMS-P937 (NMS1286937) Preparation Products And Raw materials

Raw materials

Preparation Products

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1034616-18-6, NMS-P937 (NMS1286937)Related Search:

Volasertib (BI 6727) Propylene oxide RO3280 YM155 (Sepantronium Bromide) MK-1775 GSK461364 BI 2536

NMS-1286937

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

NMS-P937 (NMS1286937)

NMS-P937

NMS-1286937,NMS-P937

1-(2-hydroxyethyl)-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide

CS-1243

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

NMS-P937 (NMS1286937) USP/EP/BP

Onvansertib（NMS-1286937

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

Onvansertib (NMS-P937)

PCM 075

PCM075

PCM-075

Onvansertib, 10 mM in DMSO

1034616-18-6

C24H27F3N8O3

Inhibitors