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SAR-020106

Catalog No. T21331 CAS 1184843-57-9

SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.

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SAR-020106, CAS 1184843-57-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 44.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 172.00
25 mg	In stock	$ 347.00
50 mg	In stock	$ 555.00
100 mg	In stock	$ 783.00
1 mL * 10 mM (in DMSO)	In stock	$ 116.00

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Purity: 97.78%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.
Targets&IC50	Chk1:13.3 nM (IC50)
In vitro	SAR-020106 potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice[2]
In vivo	SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. Cytotoxic drug combinations were associated with increased gammaH2AX and poly ADP ribose polymerase cleavage consistent with the SAR-020106-enhanced DNA damage and tumor cell death. Irinotecan and gemcitabine antitumor activity was enhanced by SAR-020106 in vivo with minimal toxicity. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility[1].

Molecular Weight	382.85
Formula	C19H19ClN6O
CAS No.	1184843-57-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12 mg/mL (31.34 mM)

References and Literature

1. Walton M I , Eve P D , Hayes A , et al. The Preclinical Pharmacology and Therapeutic Activity of the Novel CHK1 Inhibitor SAR-020106[J]. Molecular Cancer Therapeutics, 2010, 9(1):89-100. 2. Klair S , Matthews T P , Cheung K M J , et al. Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing[J]. Journal of Medicinal Chemistry, 2011, 54(24):8328-42.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library Cell Cycle Compound Library NO PAINS Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

GDC0575 monohydrochloride CCT241533 hydrochloride BML-277 M443 CCT244747 CHK-IN-1 Prexasertib dihydrochloride Rabusertib

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Keywords

SAR-020106 1184843-57-9 Cell Cycle/Checkpoint Chk SAR020106 cycle SN38 selectivity SW620 cancer inhibit colon cells SAR 020106 Checkpoint Kinase (Chk) antitumor arrest Inhibitor inhibitor

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