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Small molecules irreversibly bind to a common oncogenic mutant, K-Ras(G12C). These compounds rely on the mutant cysteine for binding and therefore do not affect the wild-type protein. Crystallographic studies reveal the formation of a new pocket that is not apparent in previous structures of Ras, beneath the effector binding switch-II region. Binding of these inhibitors to K-Ras(G12C) disrupts both switch-I and switch-II, subverting the native nucleotide preference to favour GDP over GTP and impairing binding to Raf.
| Molecular Weight | 513.78 |
| Formula | C16H21ClIN3O4S |
| CAS Number | 1469337-91-4 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Ras Products |
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| BBO-8520
BBO-8520 is a first-in-class orally active covalent KRAS G12C inhibitor. BBO-8520 inhibits KRASG12C (ON) by locking the GTP-binding protein in state 1, a conformation incapable of binding effectors, thereby inhibiting the downstream signaling of KRASG12C (ON) that promotes cell proliferation. BBO-8520 also rapidly and completely blocks the RAS-RAF1 interaction, returning KRASG12C to its inactive (OFF) state. |
| RMC-9805
RMC-9805 (KRAS G12D inhibitor 18) is an orally active KRAS G12D inhibitor. RMC-9805 (KRAS G12D inhibitor 18) inhibits RAS signaling and induces apoptosis in KRAS G12D mutant cancer cells. |
| RMC-7977
RMC-7977 is a highly selective, reversible, tri-complex RAS inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS, with affinity for both mutant and wild type (WT) variants. RMC-7977 demonstrated potent activity against RAS-addicted tumours carrying various RAS genotypes, particularly against cancer models with KRAS codon 12 mutations (KRASG12X). |
| KRpep-2d
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. |
| Rac1 Inhibitor W56
Rac1 Inhibitor W56 is a peptide containing residues 45-60 of Rac1. |
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