RMC6291

Product Name: RMC6291
CAS No.: 2641998-63-0
Chemical Name: RMC6291
Synonyms: RMC6291;elironrasib;RMC6291/ Elironrasib;Elironrasib (RMC-6291);2-(1-{1-[4-(dimethylamino)-4-methylpent-2-ynoyl]-4-fluoropiperidin-4-yl}-N-methylformamido)-N-{22-ethyl-21-[2-(1-methoxyethyl)pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-5,16-dioxa-2,10,22,28-tetraazapentacyclo[18.5.2.12,?.11?,1?.023,2?]nonacosa-1(25),20,23,26-tetraen-8-yl}-3-methylbutanamide_chiral;(3S)-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-pyridazinecarboxylic acid (3→2)-lactone;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
Formula Weight: 1012.28
MOL File: 2641998-63-0.mol

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RMC6291 Property

Density: 1.25±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml
pka: 13.33±0.40(Predicted)
form: Solid
color: White to off-white
InChIKey: HJNFYLSFWYRSHS-UHFFFAOYSA-N
SMILES: C(N1C2=CC=C3N4CCOC(CC(C(N5CCCC(N5)C(OCC(CC(C2=C3)=C1C1C=CC=NC=1C(C)OC)(C)C)=O)=O)NC(=O)C(C(C)C)N(C)C(C1(CCN(CC1)C(=O)C#CC(C)(C)N(C)C)F)=O)C4)C

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Hazard and Precautionary Statements (GHS)

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RMC6291 Chemical Properties,Usage,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

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RMC6291 Suppliers

China 45 United States 1 Global 46

Nantong QuanYi Biotechnology Co., Ltd

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2641998-63-0, RMC6291Related Search:

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)…

(3S)-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-pyridazinecarboxylic acid (3→2)-lactone

RMC6291/ Elironrasib

2-(1-{1-[4-(dimethylamino)-4-methylpent-2-ynoyl]-4-fluoropiperidin-4-yl}-N-methylformamido)-N-{22-ethyl-21-[2-(1-methoxyethyl)pyridin-3-yl]-18,18-dimethyl-9,15-dioxo-5,16-dioxa-2,10,22,28-tetraazapentacyclo[18.5.2.12,?.11?,1?.023,2?]nonacosa-1(25),20,23,26-tetraen-8-yl}-3-methylbutanamide_chiral

elironrasib

Elironrasib (RMC-6291)

2641998-63-0