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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
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 376 In Stock
5MG 416 In Stock
10MG 605 In Stock
25MG 943 In Stock
50MG 1228 In Stock
100MG 1693 In Stock
200MG 2279 In Stock
500MG Get Quote In Stock
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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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