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ATM&ATR

VE-822 (1232416-25-9)

VE-822 is an ATR inhibitor with IC50 of 19 nM.Berzosertib, also known as M6620, VE-822, VX-970, is an potent ATR inhibitor. VE-822 inhibited ATR in vitro and in vivo.

Not Intended for Therapeutic Use. For research use only.

CAS: 1232416-25-9 Category

VE-822 (1232416-25-9) Description:

Berzosertib, also known as M6620, VE-822, VX-970, is an potent ATR inhibitor. VE-822 inhibited ATR in vitro and in vivo. VE-822 decreased maintenance of cell-cycle checkpoints, increased persistent DNA damage and decreased homologous recombination in irradiated cancer cells. VE-822 decreased survival of pancreatic cancer cells but not normal cells in response to XRT or gemcitabine. VE-822 markedly prolonged growth delay of pancreatic cancer xenografts after XRT and gemcitabine-based chemoradiation without augmenting normal cell or tissue toxicity. These findings support ATR inhibition as a promising new approach to improve the therapeutic ration of radiochemotherapy for patients with PDAC.

VE-822 (1232416-25-9) Specifications:

Product Name VE-822
Synonym M6620; M-6620; M 6620; VE822; VE-822; VE 822; VX970; VX-970; VX 970; Berzosertib
Chemical Name 5-(4-(isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine.
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1232416-25-9
Molecular Formula C24H25N5O3S
Molecular Weight 463.55
Monoisotopic Mass 463.16781 g/mol
MDL number MFCD27976794
InChIKey JZCWLJDSIRUGIN-UHFFFAOYSA-N
InChi Code InChI=1S/C24H25N5O3S/c1-15(2)33(30,31)19-10-8-18(9-11-19)21-14-27-24(25)23(28-21)22-12-20(29-32-22)17-6-4-16(5-7-17)13-26-3/h4-12,14-15,26H,13H2,1-3H3,(H2,25,27)
SMILES NC1=NC=C(C2=CC=C(S(=O)(C(C)C)=O)C=C2)N=C1C3=CC(C4=CC=C(CNC)C=C4)=NO3
Form Powder
Color Yellow
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application VE-822 is an ATR inhibitor with IC50 of 19 nM.

 


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RIDADR NONH for all modes of transport

References:

[1]. Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Fokas E, Prevo R, Pollard JR, Reaper PM, Charlton PA, Cornelissen B, Vallis KA, Hammond EM, Olcina MM, Gillies McKenna W, Muschel RJ, Brunner TB. Cell Death Dis. 2012 Dec 6;3:e441. doi: 10.1038/cddis.2012.181. PMID: 23222511.

[2]. Initial testing (stage 1) of M6620 (formerly VX-970), a novel ATR inhibitor, alone and combined with cisplatin and melphalan, by the Pediatric Preclinical Testing Program. Kurmasheva RT, Kurmashev D, Reynolds CP, Kang M, Wu J, Houghton PJ, Smith MA. Pediatr Blood Cancer. 2018 Feb;65(2). doi: 10.1002/pbc.26825. Epub 2017 Sep 17. PMID: 28921800.

[3]. Small-molecule inhibitors of Ataxia Telangiectasia and Rad3 related kinase (ATR) sensitize lymphoma cells to UVA radiation. Biskup E, Naym DG, Gniadecki R. J Dermatol Sci. 2016 Dec;84(3):239-247. doi: 10.1016/j.jdermsci.2016.09.010. Epub 2016 Sep 16. PMID: 27743911.

[4]. ATR maintains chromosomal integrity during postnatal cerebellar neurogenesis and is required for medulloblastoma formation. Lang PY, Nanjangud GJ, Sokolsky-Papkov M, Shaw C, Hwang D, Parker JS, Kabanov AV, Gershon TR. Development. 2016 Nov 1;143(21):4038-4052. PMID: 27803059 Free PMC Article.

[5].Targeting ATR in cancer medicine. Sundar R, Brown J, Ingles Russo A, Yap TA. Curr Probl Cancer. 2017 Jul – Aug;41(4):302-315. doi: 10.1016/j.currproblcancer.2017.05.002. Epub 2017 May 17. Review. PMID: 28662958