A covalent inhibitor of K-RasG12C
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MRTX-1257

Item No. 33527

Technical Information
Formal Name
(2S)-1-(1-oxo-2-propen-1-yl)-4-[5,6,7,8-tetrahydro-7-(8-methyl-1-naphthalenyl)-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-2-piperazineacetonitrile
CAS Number
2206736-04-9
Molecular Formula
C33H39N7O2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/ml
λmax
226 nm
SMILES
CC1=CC=CC2=C1C(N3CC4=NC(OC[C@H]5N(C)CCC5)=NC(N6C[C@@H](N(CC6)C(C=C)=O)CC#N)=C4CC3)=CC=C2
InChi Code
InChI=1S/C33H39N7O2/c1-4-30(41)40-19-18-39(20-25(40)13-15-34)32-27-14-17-38(29-12-6-10-24-9-5-8-23(2)31(24)29)21-28(27)35-33(36-32)42-22-26-11-7-16-37(26)3/h4-6,8-10,12,25-26H,1,7,11,13-14,16-22H2,2-3H3/t25-,26-/m0/s1
InChi Key
YRYQLVCTQFBRLD-UIOOFZCWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MRTX-1257 is a covalent inhibitor of K-RasG12C.1 It inhibits proliferation of NCI H358 cells when used at concentrations ranging from 0.001 to 1 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kettle, J.G., and Cassar, D.J. Covalent inhibitors of the GTPase KRAS G12C: A review of the patent literature. Expert. OPin. Ther. Pat. 30(2), 103-120 (2020).