Home PI3K/Akt/mTOR ATM/ATR inhibitor - Chk inhibitor VX-803 (M4344) For research use only.

VX-803 (M4344)

Synonyms: ATR inhibitor 2

VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.

VX-803 (M4344) Chemical Structure

VX-803 (M4344) Chemical Structure

CAS No. 1613191-99-3

Purity & Quality Control

Batch: S963901 DMSO]15 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.99%
99.99

VX-803 (M4344) Related Products

Signaling Pathway

ATM/ATR Signaling Pathways

ATM/ATR Signaling Pathway

Biological Activity

Description VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.
Targets
ATR [1]
(Cell-free assay)		 Chk1 [1]
(Cell-free assay)
150 pM(Ki) 8 nM
In vitro
In vitro

M4344 is determined to be an adenosine triphosphate (ATP)-competitive, highly potent, and tight-binding inhibitor of ATR with a Ki of < 150 pM. Minimal inhibitory activity is observed against a large panel of unrelated protein kinases, with 308 of 312 kinases tested having a measured Ki corresponding to more than 100-fold selectivity. M4344 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with an IC50 of 8 nM. Profiling on a selected set of cancer cell lines shows synergy with several types of DNA damaging chemotherapeutics as well as PARP1/2 and CHK1 inhibitors.[1]
In Vivo
In vivo

In monotherapy efficacy studies M4344 shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression can be observed in triple-negative breast cancer xenograft models.[1]
Animal Research Animal Models Rag2 mice
Dosages 10 or 20 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04149145 Withdrawn
Ovarian Cancer Recurrent
University of Alabama at Birmingham
 May 2023 Phase 1
NCT04655183 Withdrawn
Advanced Solid Tumor|Breast Cancer
EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono
 December 1 2020 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 541.55 Formula

C25H29F2N9O3
CAS No. 1613191-99-3 SDF --
Smiles C1CN(CCC1C(=O)N2CCN(CC2)C3COC3)C4=C(C=NC=C4NC(=O)C5=C6N=CC(=CN6N=C5N)F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 15 mg/mL ( (27.69 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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