A covalent KRASG12C inhibitor
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RMC-6291

Item No. 42174

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(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
CAS Number
2641998-63-0
Molecular Formula
C55H78FN9O8
Formula Weight
1012.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C([C@H](CCC1)NN1C([C@H](C[C@H]2CN3CCO2)NC([C@H](C(C)C)N(C)C(C4(F)CCN(C(C#CC(C)(C)N(C)C)=O)CC4)=O)=O)=O)OCC(C)(C)CC5=[C@@]([C@@]6=C([C@H](C)OC)N=CC=C6)N(CC)C7=C5C=C3C=C7
InChi Code
InChI=1S/C55H78FN9O8/c1-13-64-44-19-18-37-30-40(44)41(48(64)39-16-14-24-57-46(39)36(4)71-12)32-53(5,6)34-73-51(69)42-17-15-25-65(59-42)50(68)43(31-38-33-63(37)28-29-72-38)58-49(67)47(35(2)3)61(11)52(70)55(56)22-26-62(27-23-55)45(66)20-21-54(7,8)60(9)10/h14,16,18-19,24,30,35-36,38,42-43,47,59H,13,15,17,22-23,25-29,31-34H2,1-12H3,(H,58,67)/t36-,38-,42-,43-,47-/m0/s1
InChi Key
HJNFYLSFWYRSHS-CMZSUCOPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $98

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    5 mg

    $270

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    10 mg

    $490

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    Cayman Chemical
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    Product Description

    RMC-6291 is a covalent inhibitor of KRAS containing a glycine-to-cysteine mutation at position 12 (KRASG12C).1 It binds to KRASG12C and prevents KRASG12C-induced signaling via recruitment of peptidyl-prolyl cis-trans isomerase A (PPIase A), also known as cyclophilin A (CypA). It decreases the proliferation of 15 cancer cell lines expressing KRASG12C (median EC50 = 0.11 nM) and induces apoptosis in NCI H358 non-small cell lung cancer (NSCLC) cells. RMC-6291 (10-200 mg/kg per day) reduces tumor volume in an NCI H358 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schulze, C.J., Seamon, K.J., Zhao, Y., et al. Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS. Science 381(6659), 794-799 (2023).