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Glasdegib Maleate

Cat. No. M43802
Glasdegib Maleate Structure
Synonym:

PF-04449913 Maleate

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Biological Activity

Glasdegib Maleate is an orally bioavailable Smoothened (Smo) inhibitor with an IC50 value of 4 nM for studies related to acute myeloid leukemia.

Chemical Information
Molecular Weight 490.52
Formula C25H26N6O5
CAS Number 2030410-25-2
Storage -20°C
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] Boris Peklar et al. Pharmaceutics. Glasdegib Dimaleate: Synthesis, Characterization and Comparison of Its Properties with Monomaleate Analogue

[2] Naveed Shaik et al. Cancer Chemother Pharmacol. Evaluation of the effects of formulation, food, or a proton-pump inhibitor on the pharmacokinetics of glasdegib (PF-04449913) in healthy volunteers: a randomized phase I study

[3] Nagdeep Giri et al. Cancer Chemother Pharmacol. Evaluation of the effect of new formulation, food, or a proton pump inhibitor on the relative bioavailability of the smoothened inhibitor glasdegib (PF-04449913) in healthy volunteers

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Keywords: Glasdegib Maleate, PF-04449913 Maleate supplier, Smo, inhibitors, activators


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