A covalent inhibitor of K-RasG12C
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JDQ443

Item No. 38157

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-2-propen-1-one
CAS Number
2653994-08-0
Synonyms
  • Opnurasib
Molecular Formula
C29H28ClN7O
Formula Weight
526.0
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
242 nm
SMILES
CC1=C(C2=C(C=NN3)C3=CC(C)=C2Cl)C(C4=CC(C=NN5C)=C5C=C4)=NN1C6CC7(CN(C(C=C)=O)C7)C6
InChi Code
InChI=1S/C29H28ClN7O/c1-5-24(38)36-14-29(15-36)10-20(11-29)37-17(3)25(26-21-13-31-33-22(21)8-16(2)27(26)30)28(34-37)18-6-7-23-19(9-18)12-32-35(23)4/h5-9,12-13,20H,1,10-11,14-15H2,2-4H3,(H,31,33)
InChi Key
AZUYLZMQTIKGSC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    5 mg

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    Cayman Chemical
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    Product Description

    JDQ443 is a covalent inhibitor of K-RasG12C, a mutant form of K-Ras that accumulates in cancer cells.1 It decreases K-RasG12C-induced phosphorylation of ERK in NCI H358 non-small cell lung cancer (NSCLC) cells (IC50 = 0.020 µM). JDQ443 selectively inhibits the growth of NCI H358 cells, which express K-RasG12C, over NCI H1437 NSCLC cells expressing wild-type K-Ras and the constitutively active mutant MEKQ56P (GI50s = 0.018 and 4.4 µM, respectively). It reduces blood levels of free K-RasG12C at three, six, and 24 hours in a MiaPaCa-2 pancreatic cancer mouse xenograft model when administered at a dose of 30 mg/kg and inhibits tumor growth and decreases tumor volume in the same model at 10 and 30 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lorthiois, E., Gerspacher, M., Beyer, K.S., et al. JDQ443, a structurally novel, pyrazole-based, covalent inhibitor of KRASG12C for the treatment of solid tumors. J. Med. Chem. 65(24), 16173-16203 (2022).