VE-821(VE821)cas 1232410-49-9|supplier DC Chemicals

Cas No.:	1232410-49-9
Chemical Name:	2-Pyrazinecarboxamide, 3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-
Synonyms:	VE821,VE 821
SMILES:	CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N
Formula:	C₁₈H₁₆N₄O₃S
M.Wt:	368.41
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.

In Vitro:

VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3Kγ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases[1]. VE-821 (compound 27) also inhibits ATM and DNA-PK wirh IC50 of >8 μM, and 4.4 μM, respectively[2]. VE-821 significantly enhances the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and Gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 leads to inhibition of radiation-induced G2/M arrest in cancer cells. In both PSN-1 and MiaPaCa-2 cells, 1 µM VE-821 inhibits phosphorylation of Chk1 (Ser 345) after treatment with Gemcitabine (100 nM), radiation (6 Gy) or both, at 2 h post-irradiation[3].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC3132	VE-821	VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki and IC50 of 13 nM and 26 nM, respectively.
DC7448	KU-60019	KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM.
DC1067	KU-55933	KU-55933 is a potent and specific ATM inhibitor with IC50 and Ki of 13 nM and 2.2 nM, respectively.
DC10080	GJ103 (sodium salt)	GJ103 sodium salt is an active analog of the read-through compound GJ072.
DC4112	CP466722	CP-466722 is an potent and reversible ATM inhibitor.
DC10526	BAY-1895344 HCl(Elimusertib)	BAY-1895344 is a potent and selective ATM inhibitor. BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride.
DC8468	AZD-6738	AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
DC10891	AZ-32	AZ32 is an orally bioavailable and blood-brain-barrier penetrating ATM inhibitor (AZ32) that radiosensitizes intracranial gliomas in mice.
DC10906	AZ31	AZ31 is a novel ATM inhibitor.