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Camonsertib

CAS No. 2417489-10-0

Camonsertib( —— )

Catalog No. M35617 CAS No. 2417489-10-0

Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Camonsertib
  • Note
    Research use only, not for human use.
  • Brief Description
    Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.
  • Description
    Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity.
  • In Vitro
    Western Blot AnalysisCell Line:LoVo and CW-2 human colon cancer cell lines Concentration:1 μM Incubation Time:1, 2, 4, 6, 8, 16, 24 hours Result:Inhibited CHK1(Ser345) phosphorylation from 1 to 3 hours. Starting at 4 hours, CHK1(Ser345) became re-phosphorylated as DNA-PKcs became activated in treated cells, along with its substrates KAP1 and H2AX.
  • In Vivo
    Animal Model:Female mice (6-8 weeks old) bearing LoVo xenograftsDosage:3, 7, 15 mg/kg (0.5% methylcellulose/0.02% SDS vehicle) Administration:Orally; once daily for 18 days Result:Produced dose-dependent tumor growth inhibition with a minimum effective dose (MED) of 7 mg/kg. The maximum tolerated dose (MTD) was 10 mg/kg once daily on a continuous dosing schedule.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    ATM/ATR
  • Recptor
    ATM/ATR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2417489-10-0
  • Formula Weight
    410.47
  • Molecular Formula
    C21H26N6O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (121.81 mM; Ultrasonic )
  • SMILES
    C[C@@H]1COCCN1c1cc(c2cnn(-c3cc[nH]n3)c2n1)[C@@]1(O)C[C@@H]2CC[C@H](C1)O2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Anne Roulston, et al. RP-3500: A Novel, Potent and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors. Mol Cancer Ther?
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