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RM-018

Cat. No. M11427
RM-018  Structure
Synonym:

INDEX NAME NOT YET ASSIGNED

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Biological Activity

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.

Chemical Information
Molecular Weight 985.22
Formula C56H72N8O8
CAS Number 2641993-55-5
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Noritaka Tanaka, et al. Cancer Discov. Clinical Acquired Resistance to KRAS G12C Inhibition through a Novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS-MAPK Reactivation

[2] Leslie A McSweeney, et al. Cell Microbiol. Nuclear localization of the Escherichia coli cytolethal distending toxin CdtB subunit

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  Catalog
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Keywords: RM-018 , INDEX NAME NOT YET ASSIGNED supplier, Ras, inhibitors, activators

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