Garsorasib is a potent inhibitor of KRAS G12C with an IC50 of 10 nM. Garsorasib has the potential for the research of various cancer such as pancreatic cancer, endometrial cancer, colorectal cancer, or lung cancer (non-small cell lung cancer).
Molecular Weight | 598.65 |
Formula | C32H32F2N8O2 |
CAS Number | 2559761-14-5 |
Form | Solid |
Storage | 4°C, 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.
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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
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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). |
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