533380 Sigma-AldrichPolo-like Kinase Inhibitor VI, NMS-P937 - CAS 1034616-18-6 - Calbiochem

Polo-Like Kinase Inhibitor VI, NMS-P937, CAS 1034616-18-6, is a cell-permeable, highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC₅₀ = 2 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

References
Data Sheet

Synonyms: PLK1 Inhibitor II, NMS P937, NMS-1286937

Primary Target: Plk1

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Overview

Replacement Information

Key Specifications Table

Empirical Formula	CAS #
C₂₄H₂₇F₃N₈O₃	1034616-18-6

Pricing & Availability

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Description
Overview	A cell-permeable, orally bioavailable, dihydropyrazoloquinazoline based compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC₅₀ = 2 nM). Displays excellent selectivity over Plk2 and Plk3 (IC₅₀ > 10 µM). At higher concentrations affect the activities of fms-like tyrosine kinase (Flt3), maternal embryonic leucine zipper kinase (MELK), and casein kinase 2 (IC₅₀ = 510, 744 and 826 nM, respectively). Preferentially blocks cell cycle at G2/M phase and induces apoptosis in cancer cells (IC₅₀ = 42 nM in A2780 human ovarian carcinoma cells). Shown to suppress the growth of HCT116 colon adenocarcinoma cells xenografted in CD1 nu/nu mice (45 mg/kg, b.i.d). Also exhibits good potency on taxol (Cat. No. 580555) resistant tumor cells (IC₅₀ = 65 and 62 nM for A2780 and 1A9 PTX ovarian adenocarcinoma cells, respectively). Displays desirable pharmacokinetic properties with t_1/2 = 0.9 h; AUC = 8.7 µM/h; clearance = 2.36 L/h/kg (10 mg/kg, i.v.). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number	533380
Brand Family	Calbiochem®
Synonyms	PLK1 Inhibitor II, NMS P937, NMS-1286937

References
References	Casolaro, A., et al. 2013. PLoS One 8, e58424. Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006. Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969.

Product Information
CAS number	1034616-18-6
Form	Pale yellow solid
Hill Formula	C₂₄H₂₇F₃N₈O₃
Chemical formula	C₂₄H₂₇F₃N₈O₃
Reversible	Y
Quality Level	MQ100

Applications

Biological Information
Primary Target	Plk1
Primary Target IC<sub>50</sub>	2 nM
Purity	≥98% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Documentation

References

Reference overview
Casolaro, A., et al. 2013. PLoS One 8, e58424. Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006. Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969.

Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	20-November-2015 JSW
Synonyms	PLK1 Inhibitor II, NMS P937, NMS-1286937
Description	A cell-permeable, orally bioavailable, dihydropyrazoloquinazoline based compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC₅₀ = 2 nM). Displays excellent selectivity over Plk2 and Plk3 (IC₅₀ > 10 µM). At higher concentrations affect the activities of fms-like tyrosine kinase (Flt3), maternal embryonic leucine zipper kinase (MELK), and casein kinase 2 (IC₅₀ = 510, 744 and 826 nM, respectively). Preferentially blocks cell cycle at G2/M phase and induces apoptosis in cancer cells (IC₅₀ = 42 nM in A2780 human ovarian carcinoma cells). Shown to suppress the growth of HCT116 colon adenocarcinoma cells xenografted in CD1 nu/nu mice (45 mg/kg, b.i.d). Also exhibits good potency on taxol (Cat. No. 580555) resistant tumor cells (IC₅₀ = 65 and 62 nM for A2780 and 1A9 PTX ovarian adenocarcinoma cells, respectively). Displays desirable pharmacokinetic properties with t_1/2 = 0.9 h; AUC = 8.7 µM/h; clearance = 2.36 L/h/kg (10 mg/kg, i.v.).
Form	Pale yellow solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1034616-18-6
Chemical formula	C₂₄H₂₇F₃N₈O₃
Purity	≥98% by HPLC
Solubility	DMSO (10 mg/ml)
Storage	+2°C to +8°C Protect from light
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	Casolaro, A., et al. 2013. PLoS One 8, e58424. Valsasina, B., et al. 2012. Mol. Cancer Ther.11, 1006. Beria, I., et al. 2011. Bioorg. Med. Chem. Lett. 21, 2969.