RMC6291
- CAS No.
- 2641998-63-0
- Chemical Name:
- RMC6291
- Synonyms
- RMC6291;3-Pyridazinecarboxylic acid, N1-[N-[[1-[4-(dimethylamino)-4-methyl-1-oxo-2-pentyn-1-yl]-4-fluoro-4-piperidinyl]carbonyl]-N-methyl-L-valyl-3-[4-[(2R)-1-ethyl-3-(3-hydroxy-2,2-dimethylpropyl)-2-[2-[(1S)-1-methoxyethyl]-3-pyridinyl]-1H-indol-5-yl]-2-morpholinyl]-L-alanyl]hexahydro-, (3→2)-lactone, (3S)…
- CBNumber:
- CB113267341
- Molecular Formula:
- C55H78FN9O8
- Molecular Weight:
- 1012.28
- MDL Number:
- MOL File:
- 2641998-63-0.mol
RMC6291 Chemical Properties,Uses,Production
Uses
Elironrasib is an orally active and covalent inhibitor of KRASG12C(ON). Elironrasib forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRASG12C mutant cells with a median IC50 of 0.11 nM[1][2].
in vivo
Elironrasib (200mg/kg, p.o., qd for 60 d) significantly inhibits tumor growth and induce immunological memory in murine tumor models[3].
IC 50
KRAS(G12C)
References
[1] Nichols R J, et al. RMC-6291, a next-generation tri-complex KRASG12C (ON) inhibitor, outperforms KRASG12C (OFF) inhibitors in preclinical models of KRASG12C cancers[J]. Cancer Research, 2022, 82(12_Supplement): 3595-3595.
[2] Schulze CJ, et al. Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS. Science. 2023 Aug 18;381(6659):794-799. DOI:10.1126/science.adg9652
[3] Cristina Blaj, et al. Enhancement of anti-tumor immunity in immunogenic and immune-refractory RAS mutant tumors with tri-complex RAS(ON) inhibitors, revmed, #PB044, 2022
RMC6291 Preparation Products And Raw materials
Raw materials
Preparation Products
RMC6291 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5237 | 58 |
| Beijing Yaoxuan Technology Co.,Ltd. | 13141108551 | Novochem@163.com | China | 50 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4351 | 58 |
| Suzhou Haiben Pharmaceutical Co., Ltd | 14760821013 13564957716 | 1816280386@qq.com | China | 8045 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4601 | 55 | |
| Shanghaizehan biopharma technology co., Ltd. | 021-61350663 13052117465 | sales@zehanbiopharma.com | China | 996 | 55 |
| Shanghai Chaolan Chemical Technology Center | 021-QQ：65489617 15618227136 | Sales@ATKchemical.com | China | 9330 | 58 |
| Perida Pharmaceutical Co., Ltd. | 010-87568995 13439954790 | 2539095144@qq.com | China | 210 | 58 |
| Shanghai Tube Pharmaceutical Co., Ltd. | 021-54338626 18017892860 | sales@tubepharm.com | China | 2511 | 58 |
