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ARS-1323 is a novel inhibitor of mutant K-ras G12C.
| 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 | 430.84 |
| Formula | C21H17ClF2N4O2 |
| CAS Number | 1698024-73-5 |
| Purity | >98% |
| Solubility | DMSO: ≥ 60 mg/mL |
| Storage | at -20°C |
[1] Peter D Koch, et al. SMALL MOLECULE IMAGING AGENT FOR MUTANT KRAS G12C
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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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