A K-RasG12C inhibitor
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Garsorasib

Item No. 44250

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-(2-amino-6-fluorophenyl)-1-(4, 6-dicyclopropyl-5-pyrimidinyl)-4-[(2S,5R)-2,5-dimethyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-6-fluoro-pyrido[2,3-d]pyrimidin-2(1H)-one
CAS Number
2559761-14-5
Synonyms
  • D-1553
Molecular Formula
C32H32F2N8O2
Formula Weight
598.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1N(C2=NC(C3=C(C=CC=C3N)F)=C(F)C=C2C(N4[C@H](CN([C@@H](C4)C)C(C=C)=O)C)=N1)C5=C(C6CC6)N=CN=C5C7CC7
InChi Code
InChI=1S/C32H32F2N8O2/c1-4-24(43)40-13-17(3)41(14-16(40)2)30-20-12-22(34)28(25-21(33)6-5-7-23(25)35)38-31(20)42(32(44)39-30)29-26(18-8-9-18)36-15-37-27(29)19-10-11-19/h4-7,12,15-19H,1,8-11,13-14,35H2,2-3H3/t16-,17+/m1/s1
InChi Key
DKFRWZJCNPETGI-SJORKVTESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $96

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    5 mg

    $432

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    Product Description

    Garsorasib is an inhibitor of K-Ras containing the activating glycine-to-cysteine mutation at position 12 (K-RasG12C; IC50 = 18 nM).1 It selectively binds to GDP-bound K-RasG12C over GDP-bound wild-type K-Ras in thermal shift assays and selectively inhibits ERK phosphorylation in NCI H358 cells, which express K-RasG12C, over NCI H1993 cells, which express wild-type K-Ras (IC50s = 6.9 and >1,000 nM, respectively). Garsorasib inhibits proliferation in 11 K-RasG12C-expressing cancer cell lines (IC50s = 4.6-33 nM) but not in K-RasG12D- or wild-type-expressing cancer cells (IC50s = >10,000 nM). In vivo, garsorasib (30 mg/kg) induces tumor regression in NCI H358 non-small cell lung cancer (NSCLC) and MIA PaCa-2 pancreatic cancer mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shi, Z., Weng, J., Niu, H., et al. D-1553: A novel KRASG12C inhibitor with potent and selective cellular and in vivo antitumor activity. Cancer Sci. 114(7), 2951-2960 (2023).