VRX-0466617|VRX 0466617;VRX0466617

Cas No.:	926906-64-1
Chemical Name:	5-[4-(4-Bromoanilino)anilino]-N'-(1-hydroxypropan-2-yl)-3-oxo-1,2-thiazole-4-carboximidamide
Synonyms:	VRX 0466617;VRX0466617
SMILES:	S1C(NC2=CC=C(NC3=CC=C(Br)C=C3)C=C2)=C(/C(/N)=N/C(C)CO)C(=O)N1
Formula:	C₁₉H₂₀BrN₅O₂S
M.Wt:	462.366
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM; shows no inhibitory effect on Chk1 (>100 uM); inhibits the phosphorylation of Chk2 Ser(19) and Ser(33-35), but not of Chk2 Thr(68), prevents the IR-induced Chk2-dependent degradation of Hdmx and attenuates IR-induced apoptosis.

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.