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K-Ras(G12C) inhibitor 9

Cat. No. M3663
K-Ras(G12C) inhibitor 9 Structure
Size Price Availability Quantity
2mg USD 94.5  USD105 In stock
5mg USD 139.5  USD155 In stock
10mg USD 220.5  USD245 In stock
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Quality Control
Biological Activity

Small molecules irreversibly bind to a common oncogenic mutant, K-Ras(G12C). These compounds rely on the mutant cysteine for binding and therefore do not affect the wild-type protein. Crystallographic studies reveal the formation of a new pocket that is not apparent in previous structures of Ras, beneath the effector binding switch-II region. Binding of these inhibitors to K-Ras(G12C) disrupts both switch-I and switch-II, subverting the native nucleotide preference to favour GDP over GTP and impairing binding to Raf.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 513.78
Formula C16H21ClIN3O4S
CAS Number 1469337-91-4
Purity 98.81%
Solubility DMSO: ≥ 40 mg/mL
Storage at -20°C
References

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions.
Ostrem JM, et al. Nature. 2013 Nov 28;503(7477):548-51. PMID: 24256730.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: K-Ras(G12C) inhibitor 9 supplier, Ras, inhibitors

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