BI-3406 is a highly potent and selective SOS1::KRAS inhibitor (IC50=6 nM), which selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation. BI 3406 causes RAS GTP and pERK reduction and inhibits cell growth of KRAS mutated cell lines, carrying most of the typical KRAS mutations (i.e. G12D, G12V, G13D and others). BI 3406, when administered orally to tumour bearing mice, causes a dose dependent tumour static effect.
| Molecular Weight | 462.46 |
| Formula | C23H25F3N4O3 |
| CAS Number | 2230836-55-0 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage | 2-8°C, dry, protect from light, sealed |
| 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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| 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. |
| SAH-SOS1A
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. |
| Glecirasib
Glecirasib is a potent, irreversible, orally active KRAS G12C inhibitor for studies related to KRAS G12C-mediated cancers. |
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