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PF-562771

Cat. No. M3778
PF-562771 Structure
Synonym:

AP23848

Size Price Availability
5mg USD 120  USD120 Custom Synthesis
10mg USD 190  USD190 Custom Synthesis
50mg USD 660  USD660 Custom Synthesis
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Quality Control & Documentation
Biological Activity

AP23464 and PF-562771 (AP23848) potently and selectively target activation-loop mutants of Kit in vitro and in vivo and could have therapeutic potential against D816V-expressing malignancies. Src/Abl inhibitors are compatible with imatinib and suggest that combined Abl inhibitor therapy is a feasible treatment strategy for patients with CML.

Chemical Information
Molecular Weight 531.63
Formula C30H38N5O2P
CAS Number 834894-21-2
Solubility (25°C) DMSO 10 mM
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] O'Hare T, et al. Clin Cancer Res. Combined Abl inhibitor therapy for minimizing drug resistance in chronic myeloid leukemia: Src/Abl inhibitors are compatible with imatinib.

[2] Corbin AS, et al. Blood. In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-562771, AP23848 supplier, Src-bcr-Abl, inhibitors, activators


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