A covalent inhibitor of K-RasG12C
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GDC-6036

Item No. 41852

Technical Information
Formal Name
1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]-2-propen-1-one
CAS Number
2417987-45-0
Synonyms
  • Divarasib
  • RG-6330
Molecular Formula
C29H32ClF4N7O2
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: Soluble: ≥10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
CN(CCC1)C1COC2=NC(N3C(C)CN(C(C=C)=O)CC3)=C(C=C(C(C4=C(C(F)(F)F)C(C)=CC(N)=N4)=C5F)Cl)C5=N2
InChi Code
InChI=1S/C29H32ClF4N7O2/c1-5-21(42)40-9-10-41(16(3)13-40)27-18-12-19(30)22(26-23(29(32,33)34)15(2)11-20(35)36-26)24(31)25(18)37-28(38-27)43-14-17-7-6-8-39(17)4/h5,11-12,16-17H,1,6-10,13-14H2,2-4H3,(H2,35,36)
InChi Key
ZRBPIAWWRPFDPY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GDC-6036 is a covalent inhibitor of K-Ras containing a glycine-to-cysteine substitution at position 12 (K-RasG12C).1 It decreases tumor volume in a PaCa-2 pancreatic cancer mouse xenograft model when administered at doses ranging from 1 to 100 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tran, J.C., Hunsaker, T., Bell, C., et alQuantifying KRAS G12C covalent drug inhibitor activity in mouse tumors using mass spectrometry. Anal. Chem. 95(11), 4834-4839 (2023).