BDP9066 is a selective and potent inhibitor of myotonic dystrophy-associated Cdc-42-binding kinase MRCK, with an IC50 value of 64 nM for MRCKβ and Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β, respectively, measured in SCC12 cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO : 10 mg/mL|
|Related Ras Products|
BI-0474 is a covalent KRASG12C inhibitor. The IC50 value for GDP-KRAS::SOS1 protein-protein interaction was 7.0 nM. BI-0474 also showed better antitumor activity in non-small cell lung cancer xenograft models.
MRTX849 acid can be used to synthesize PROTAC LC-2. LC-2 is a potent, first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50, between 0.25 and 0.76 μM).
ASP2453 is a potent, selective and covalent inhibitor of KRAS G12C. ASP2453 inhibits Son of Sevenless (SOS)-mediated interactions between KRAS G12C and Raf with an IC50 value of 40 nM.
AZD4625 is a highly potent, selective, covalent and metabotropic inhibitor of the mutant GTPase KRASG12C. AZD4625 has high oral bioavailability. It is being developed to study advanced solid malignancies.
Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
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