VE-822, also known as VX-970 or Berzosertib, 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.

MedKoo Cat#: 406258 Name: VE-822 (VX-970) CAS#: 1232416-25-9 Chemical Formula: C24H25N5O3S Exact Mass: 463.16781 Molecular Weight: 463.55 Elemental Analysis: C, 62.18; H, 5.44; N, 15.11; O, 10.35; S, 6.92

Synonym: VE822; VE-822; VE 822; VX970; VX-970; VX 970; Berzosertib

IUPAC/Chemical Name: 5-(4-(isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine.

InChi Key: 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 Code: NC1=NC=C(C2=CC=C(S(=O)(C(C)C)=O)C=C2)N=C1C3=CC(C4=CC=C(CNC)C=C4)=NO3

Technical Data

Appearance: Yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Certificate of Analysis: View CoA: previous batch: lot#BBC20130911 View CoA: previous batch, lot#SSC40215 View CoA: current batch, Lot#S7S05C02

QC Data: View QC data: previous batch, lot#BBC20130911 View QC data: previous batch, lot#SSC40215 View QC data: current batch, Lot#S7S05C02

Safety Data Sheet (MSDS): View Material Safety Data Sheet (MSDS)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: For in vivo study, VE-822 can be formulated in DMSO. For the in vivo studies, VE-822 was dissolved in 10% Vitamin E d-alpha tocopheryl polyethylene glycol 1000 succinate and administered by gavage, in 200μl.

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

        

References

1: 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. Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Cell Death Dis. 2012 Dec 6;3:e441. doi: 10.1038/cddis.2012.181. PubMed PMID: 23222511; PubMed Central PMCID: PMC3542617.

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