Onvansertib

SKU: orb1300940

Description

Onvansertib (NMS-1286937) is a potent, selective, and orally bioavailable inhibitor of Polo-like kinase 1 (PLK1) with an IC50 of 2 nM. It demonstrates antitumor activity by inhibiting cancer cell proliferation in vitro and suppressing tumor growth in various in vivo xenograft models.

Research Area

Cell Biology

Images & Validation

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Key Properties

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CAS Number	1034616-18-6
MW	532.52
Purity	97.01% (May vary between batches)
Formula	C₂₄H₂₇F₃N₈O₃
SMILES	CN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(CCO)c4-c3n2)C(N)=O)c1
Target	PLK,Apoptosis
Solubility	Ethanol:10 mg/mL (18.78 mM);DMSO:25 mg/mL (46.95 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.76 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	CK2:826 nM\|PLK1:2 nM\|MELK:744 nM\|FLT3:510 nM
In Vivo	METHODS: To test the antitumor activity in vivo, Onvansertib (60 mg/kg) was administered orally to Hsd, athymic nu/nu mice bearing HCT116 xenografts once daily for eight days. RESULTS: Onvansertib was able to achieve good antitumor activity with minimal weight loss and inhibited tumor growth to a considerable extent with a TGI of 79%. Read more...
In Vitro	METHODS: 137 tumor cells were treated with Onvansertib for 72 h. Cell viability was measured by CellTiter-Glo Assay. RESULTS: Sixty of the 137 cell lines had IC50 values below 100 nmol/L, and only 9 cell lines had IC50 values above 1 µmol/L, indicating a wide range of activity. METHODS: Cisplatin-sensitive and -resistant CAL33 were treated with Onvansertib (25-50 nM) for 24 days, and the cell cycle was examined by Flow cytometry. RESULTS: Onvansertib treatment induced accumulation of all sensitive and resistant CAL33 cells in G2/M phase in a dose-dependent manner. Read more...
Cell Research	Cells are seeded into 96- or 384-well plates at densities ranging from 10,000 to 30,000/cm2 for adherent and 100,000/mL for nonadherent cells in appropriate medium supplemented with 10% fetal calf serum. After 24 hours, cells were treated in duplicate with serial dilutions of NMS-P937, and 72 hours later, the viable cell number was assessed by the CellTiter-Glo Assay (Promega). IC50 values were calculated with a sigmoidal fitting algorithm (Assay Explorer MDL). Experiments were carried out independently at least twice.(Only for Reference) Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Apoptosis, inhibit, PLK, PLK3, PLK1, PLK2, Onvansertib, NMS-P937, NMS-P-937, NMS1286937, NMS-1286937, NMS-P 937, NMS 1286937, Inhibitor, Polo-like Kinase (PLK)

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Compound Identifiers

PubChem CID

49792852 ↗

Key Properties

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No computed properties available.

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Onvansertib (orb1300940)

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Purity:	>98%
CAS Number:	1263293-37-3
MW:	648.6
Formula:	C₂₈H₃₁F₃N₈O₇

Purity:	>98% (HPLC)
CAS Number:	1034616-18-6
MW:	532.52
Formula:	C₂₄H₂₇F₃N₈O₃

Onvansertib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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