2417987-45-0
Chemical Structure
Divarasib
Synonym(s): GDC-6036
- CAS No.: 2417987-45-0
- Formula:C29H32ClF4N7O2
- Molecular Weight:622.06
IUPAC Name: ((((((5-(bromomethyl)-1,3-phenylene)bis(oxy))bis(methylene))bis(benzene-5,1,3-triyl))tetrakis(oxy))tetrakis(methylene))tetrabenzene
InChIKey: ZRBPIAWWRPFDPY-IRXDYDNUSA-N
SMILES: NC1=N[C@]([C@]2=C(C=C3C(N=C(N=C3N4[C@H](CN(CC4)C(C=C)=O)C)OC[C@H]5N(CCC5)C)=C2F)Cl)=C(C(C)=C1)C(F)(F)F
Biological Activity: Divarasib (GDC-6036) is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors[1][2][3][4].
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Divarasib | 99.31% | Divarasib (GDC-6036) is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors. | ||||||||||||||||||||
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- [1]. Meng L, et al. Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC-MS/MS Approach. Anal Chem. 2022 Sep 20;94(37):12927-12933. [Content Brief]
- [2]. Endres NF, et al. Discovery and Characterization of Divarasib (GDC-6036), a Potent Covalent Inhibitor of KRAS G12C. J Med Chem. 2026;69(5):5147-5165. [Content Brief]
- [3]. Brazel D, et al. Divarasib in the Evolving Landscape of KRAS G12C Inhibitors for NSCLC. Target Oncol. 2024;19(3):297-301. [Content Brief]
- [4]. Jayesh Desai, et al. Abstract CT029: Phase Ib study of GDC-6036 in combination with cetuximab in patients with colorectal cancer (CRC) with KRAS G12C mutation. Cancer Res (2023) 83 (8_Supplement): CT029.
Keywords
