SAR-020106|SAR 020106;SAR020106

Cas No.:	184843-57-9
Chemical Name:	(R)-5-((8-chloroisoquinolin-3-yl)amino)-3-((1-(dimethylamino)propan-2-yl)oxy)pyrazine-2-carbonitrile
Synonyms:	SAR 020106;SAR020106
SMILES:	C(C#N)1=NC=C(NC2=CC3=C(C=N2)C(Cl)=CC=C3)N=C1O[C@@H](C)CN(C)C
Formula:	C₁₉H₁₉ClN₆O
M.Wt:	382.85
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM; brogates the etoposide-induced G(2) arrest with IC50 of 55 nM in HT29 cells, significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro; inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 both in vitro and in vivo; enhances irinotecan and gemcitabine antitumor activity in mice with minimal toxicity.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC41105	Prexasertib dimesylate	Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
DC41104	Prexasertib Mesylate Hydrate	Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.
DC40569	Chk1-IN-5	Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
DC11732	GNE-900	GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM.
DC9399	CCT241533 (hydrochloride)	CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM.
DC11713	NSC-109555 ditosylate	A potent, selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 uM.
DC11733	SAR-020106	A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.
DC11711	VER-158411	A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
DC11717	PD-321852	A potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM.
DC11714	PV-1019	A potent, ATP-competitive and highly selective Chk2 inhibitor with IC50 of 138 nM.