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K-Ras(G12C) inhibitor 6

Cat. No. M20596
K-Ras(G12C) inhibitor 6 Structure
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Biological Activity

K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).

Chemical Information
Molecular Weight 405.34
Formula C17H22Cl2N2O3S
CAS Number 2060530-16-5
Solubility (25°C) DMSO 81 mg/mL
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] Kotaro Sakamoto, et al. Sci Rep. The K-Ras(G12D)-inhibitory peptide KS-58 suppresses growth of murine CT26 colorectal cancer cell-derived tumors

[2] Heike Jger, et al. Mol Pharmacol. Blockage of intermediate-conductance Ca2+-activated K+ channels inhibit human pancreatic cancer cell growth in vitro

[3] Jung Rock Moon, et al. Int J Oncol. TGF-β1 protects colon tumor cells from apoptosis through XAF1 suppression

[4] Khuchtumur Bum-Erdene, et al. ChemMedChem. Covalent Fragment Screening Identifies Rgl2 RalGEF Cysteine for Targeted Covalent Inhibition of Ral GTPase Activation

[5] Ping-Chih Hsu, et al. J Cell Mol Med. Inhibition of yes-associated protein suppresses brain metastasis of human lung adenocarcinoma in a murine model

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