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Selumetinib sulfate

Cat. No. M14171
Selumetinib sulfate Structure
Synonym:

AZD6244 sulfate; ARRY-142886 sulfate

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Quality Control & Documentation
Biological Activity

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

Chemical Information
Molecular Weight 555.76
CAS Number 943332-08-9
Storage 2-8°C, dry, sealed
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] Evgeny N Imyanitov, et al. Treating non-small cell lung cancer with selumetinib: an up-to-date drug evaluation

[2] Richard D Carvajal, et al. Selumetinib in Combination With Dacarbazine in Patients With Metastatic Uveal Melanoma: A Phase III, Multicenter, Randomized Trial (SUMIT)

[3] Giulio Metro, et al. Selumetinib: a promising pharmacologic approach for KRAS-mutant advanced non-small-cell lung cancer

[4] A Tomillero, et al. Gateways to clinical trials

[5] A Tomillero, et al. Gateways to clinical trials

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  Catalog
Abmole Inhibitor Catalog




Keywords: Selumetinib sulfate, AZD6244 sulfate; ARRY-142886 sulfate supplier, MEK, inhibitors, activators


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