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Garsorasib

Chemical Structure : Garsorasib

CAS No.: 2559761-14-5

Garsorasib (D-1553, D1553)

Catalog No.: PC-73419Not For Human Use, Lab Use Only.

Garsorasib (D-1553) is a potent, selective, orally bioavailable and covalent KRas-G12C inhibitor with IC50 of 10 nM, exhibits potent anti-tumor activity in a broad spectrum of tumor cell lines.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Garsorasib (D-1553) is a potent, selective, orally bioavailable and covalent KRas-G12C inhibitor with IC50 of 10 nM, exhibits potent anti-tumor activity in a broad spectrum of tumor cell lines.
Garsorasib (D-1553) shows specific activity in cancer cells with KRas-G12C mutation, including lung, pancreatic and colorectal cancers.
Garsorasib (D-1553) is highly potent in vivo in various cell line-derived xenograft tumor models with KRas-G12C mutation as a single agent.
Garsorasib (D-1553) demonstrates further tumor growth inhibition or regression in tumor xenograft models, when combined with MEK inhibitor, SHP2 inhibitor or cytotoxic agents.
Garsorasib (D-1553) has anti-tumor activity in a broad spectrum of cancers and is suitable for tissue-agnostic clinical development targeting cancers with KRas-G12C mutation.

Physicochemical Properties

M.Wt 598.659
Formula C32H32F2N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7-(2-amino-6-fluorophenyl)-1-(4,6- dicyclopropylpyrimidin-5-yl)-4-[(2S,5R)-2,5-dimethyl-4- (prop-2-enoyl)piperazin-1-yl]-6-fluoropyrido[2,3- d]pyrimidin-2(1H)-one

References

1. Albert K Kwan, et al. J Exp Clin Cancer Res. 2022 Jan 19;41(1):27.

2. Zhe Shi, et al. Cancer Res (2021) 81 (13_Supplement): 932.

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