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Divarasib

CAS No. 2417987-45-0

Divarasib( —— )

Catalog No. M37705 CAS No. 2417987-45-0

Divarasib (GDC-6036) (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of < 0.01 μM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Divarasib
  • Note
    Research use only, not for human use.
  • Brief Description
    Divarasib (GDC-6036) (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of < 0.01 μM.
  • Description
    Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Female C.B-17 SCID (Inbred) mice (20-21 weeks old; 24.1 g) with human NSCLC NCI-H2030.X1.1 cellsDosage:10, 25, or 100 mg/kg Administration:Oral gavage (PO) every day (QD) for 7 days (vehicle: 0.5% methylcellulose)Result:Decreased the ratio of free KRAS G12C to internal standard. Dose-dependent target engagement was observed for all time points (2, 8, and 24 h post-last dose), with over 90% KRAS G12C engagement observed for the highest dose 100 mg/kg assessed.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Kras
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2417987-45-0
  • Formula Weight
    622.06
  • Molecular Formula
    C29H32ClF4N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (160.76 mM; Ultrasonic )
  • SMILES
    C[C@H]1CN(CCN1c1nc(OC[C@@H]2CCCN2C)nc2c(F)c(c(Cl)cc12)-c1nc(N)cc(C)c1C(F)(F)F)C(=O)C=C
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Lingyao Meng, et al. Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC-MS/MS Approach. Anal Chem. 2022 Sep 20;94(37):12927-12933.?
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