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Masitinib mesylate

Cat. No. M10665
Masitinib mesylate Structure
Synonym:

AB-1010 mesylate

Size Price Availability Quantity
10mg USD 50  USD50 In stock
50mg USD 110  USD110 In stock
100mg USD 165  USD165 In stock
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Quality Control
Biological Activity

Masitinib (AB-1010) mesylate is a potent, orally bioavailable and selective inhibitor of c-Kit, IC50 of 200 nM for human recombinant c-Kit. It also inhibits PDGFRα/β, LynB with IC50 values of 540, 800 and 510 nM. In Ba/F3 cells expressing human wild-type Kit, masitinib inhibits SCF (stem cell factor)-induced cell proliferation with an IC50 of 150 nM, while the IC50 for inhibition of IL-3-stimulated proliferation is at approximately >10 µM. In Ba/F3 cells expressing PDGFRα, masitinib inhibits PDGF-BB-stimulated proliferation and PDGFRα tyrosine phosphorylation with IC50 of 300 nM. Masitinib also causes inhibition of SCF-stimulated tyrosine phosphorylation of human Kit in mastocytoma cell-lines and BMMC.

In vivo, Masitinib inhibits tumour growth and increases the median survival time in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity or genotoxicity.

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 594.75
Formula C29H34N6O4S2
CAS Number 1048007-93-7
Purity 99.94%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C
References

[1] Ilaria Marech, et al. Crit Rev Oncol Hematol . Masitinib (AB1010), from canine tumor model to human clinical development: where we are

[2] J Lawrence, et al. Vet Comp Oncol . Masitinib demonstrates anti-proliferative and pro-apoptotic activity in primary and metastatic feline injection-site sarcoma cells

[3] Patrice Dubreuil, et al. PLoS One . Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Masitinib mesylate, AB-1010 mesylate supplier, c-Kit, inhibitors

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