A covalent K-RasG12C inhibitor
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Glecirasib

Item No. 45041

Technical Information
Formal Name
7-(2-amino-3,4,5,6-tetrafluorophenyl)-6-chloro-1,2-dihydro-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-2-oxo-4-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-1,8-naphthyridine-3-carbonitrile
CAS Number
2657613-87-9
Molecular Formula
C31H26ClF4N7O2
Formula Weight
Purity
≥98%
A solid
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
FC(C(C1=NC(N2C3=C(C=CN=C3C(C)C)C)=C(C=C1Cl)C(N4CCN(CC4)C(C=C)=O)=C(C#N)C2=O)=C(N)C(F)=C5F)=C5F
InChi Code
InChI=1S/C31H26ClF4N7O2/c1-5-19(44)41-8-10-42(11-9-41)29-16-12-18(32)27(20-21(33)22(34)23(35)24(36)25(20)38)40-30(16)43(31(45)17(29)13-37)28-15(4)6-7-39-26(28)14(2)3/h5-7,12,14H,1,8-11,38H2,2-4H3
InChi Key
QRRJEUIQLZNPIO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Glecirasib is a covalent inhibitor of K-Ras containing the activating glycine-to-cysteine mutation at position 12 (K-RasG12C; IC50 = 1.6 nM).1 It inhibits ERK phosphorylation in K-RasG12C-expressing NCI H358 non-small cell lung cancer (NSCLC) cells (IC50 = 7.3 nM) and reduces their viability (IC50 = 23 nM). In vivo, glecirasib (10 mg/kg) inhibits tumor growth in an NCI H1373 NSCLC mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, A., Li, S., Wang, P., et alDesign, structure optimization, and preclinical characterization of JAB-21822, a covalent inhibitor of KRASG12C. J. Med. Chem. 68(3), 2422-2436 (2025).