PROTAC KRAS G12C degrader-1

• CAT Number: I044438
• CAS Number: 2984236-79-3
• Molecular Formula: C50H54ClFN8O6
• Molecular Weight: 917.47
• Purity: ≥95%
• Synonyms: 4-[12-[[6-chloro-8-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(4-prop-2-enoylpiperazin-1-yl)quinazolin-2-yl]amino]dodecylamino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
• InChI: InChI=1S/C50H54ClFN8O6/c1-2-41(63)58-24-26-59(27-25-58)46-36-30-37(51)42(35-29-32(61)28-31-16-11-12-17-33(31)35)44(52)45(36)56-50(57-46)54-23-14-10-8-6-4-3-5-7-9-13-22-53-38-19-15-18-34-43(38)49(66)60(48(34)65)39-20-21-40(62)55-47(39)64/h2,11-12,15-19,28-30,39,53,61H,1,3-10,13-14,20-27H2,(H,54,56,57)(H,55,62,64)
• InChIKey: FMYAMLPDKZOVMB-UHFFFAOYSA-N
• SMILES: C=CC(=O)N1CCN(CC1)C2=NC(=NC3=C(C(=C(C=C32)Cl)C4=CC(=CC5=CC=CC=C54)O)F)NCCCCCCCCCCCCNC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O

PROTAC KRAS G12C degrader-1 is a Cereblon-based KRASG12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRASG12C dimerization and degrades GFP- KRASG12C in reporter cells[1].
PROTAC KRAS G12C degrader-1 (Compound 10) engages CRBN in cells, bound KRASG12C in vitro, induces CRBN/KRASG12C dimerization, and degrades GFP-KRASG12C in reporter cells in a CRBN-dependent manner[1].

Reference

[1]. Zeng M, et, al. Exploring Targeted Degradation Strategy for Oncogenic KRAS G12C. Cell Chem Biol. 2020 Jan 16;27(1):19-31.e6.
 [Content Brief]