AMG-510 (Sotorasib) selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant.
In preclinical tumor models, AMG 510 rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. AMG 510 (orally, once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer.
iScience. 2023 Jan 28;26(2):106080..
Global profiling of AMG510 modified proteins identified tumor suppressor KEAP1 as an off-target
AMG-510 (Sotorasib) purchased from AbMole
Molecular Weight | 560.59 |
Formula | C30H30F2N6O3 |
CAS Number | 2296729-00-3 |
Solubility (25°C) | DMSO ≥ 50 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.
[2] David S Hong, et al. KRAS G12C Inhibition with Sotorasib in Advanced Solid Tumors
[3] No authors listed. Cancer Discov. AMG 510 Shows Activity beyond NSCLC
[5] Jude Canon, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity
Related Ras Products |
---|
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.