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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.
| 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.
| Molecular Weight | 462.46 |
| Formula | C23H25F3N4O3 |
| CAS Number | 2230836-55-0 |
| Purity | >98% |
| Solubility | DMSO ≥ 90 mg/mL |
| Storage | 2-8°C, dry, protect from light, sealed |
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| MRTX0902
MRTX0902 is an effective SOS1 inhibitor with an IC50 of 46 nM. |
| GDC-6036
Gdc-6036 (compound 17A) is an oral covalently mutated KRAS G12C inhibitor with IC50<0.01 μM against K-Ras G12C. The EC50 of GDC-6036 in K-Ras G12C-alkylated HCC1171 cells was 2 nM. |
| RM-018
RM-018 is an inhibitor of the active state of KRASG12C. Rm-018 retains the ability to bind and inhibit KRASG12C/Y96D. Rm-018 combines with GTP-bound to activate the [" RAS(ON) "] state of KRASG12C. |
| HJC0197
HJC0197 is a potent antagonist of Epac1 (the exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2). HJC0197 selectively blocked camp-induced Epac activation. HJC0197 inhibited epAC1-mediated RAP1-GDP exchange activity in the presence of isoconcentration of cAMP. |
| SAH-SOS1A TFA
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM) and directly and independently blocks nucleotide association. |
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