An allosteric inhibitor of oncogenic K-Ras(G12C)
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K-Ras(G12C) Inhibitor 12

Item No. 20118

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[2-[(4-chloro-2-hydroxy-5-iodophenyl)amino]acetyl]-1-piperazinyl]-2-propen-1-one
CAS Number
1469337-95-8
Synonyms
  • K-Ras4A(G12C) Inhibitor 12
  • c-K-ras(G12C) Inhibitor 12
  • Ki-Ras(G12C) Inhibitor 12
  • c-Ki-ras(G12C) Inhibitor 12
  • KRAS(G12C) Inhibitor 12
  • Kristen Rat Sarcoma Virus(G12C) Inhibitor 12
Molecular Formula
C15H17ClIN3O3
Formula Weight
449.7
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 0.33 mg/ml
λmax
220, 254, 307 nm
SMILES
IC1=C(Cl)C=C(O)C(NCC(N2CCN(C(C=C)=O)CC2)=O)=C1
InChi Code
InChI=1S/C15H17ClIN3O3/c1-2-14(22)19-3-5-20(6-4-19)15(23)9-18-12-8-11(17)10(16)7-13(12)21/h2,7-8,18,21H,1,3-6,9H2
InChi Key
JFIFBWVNHLXJFY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    K-Ras(G12C) inhibitor 12 irreversibly binds to the oncogenic mutant K-Ras(G12C), blocking K-Ras(G12C) interactions.1 K-Ras is a small GTPase that cycles between a GTP-bound active state and a GDP-bound inactive state to turn on downstream Raf kinases to drive cell growth. A G12C mutation in K-Ras blocks GTP hydrolysis, activates K-Ras, and promotes carcinogenesis. This compound has been used to decrease viability and increase apoptosis in several lung cancer cell lines containing G12C mutations (EC50 = 0.32 µM in H1792 cells).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ostrem, J.M., Peters, U., Sos, M.L., et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature 503(7477), 548-551 (2013).