Masitinib (AB1010)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 1g | $650 | Check With Us |
| 2g | $900 | Check With Us |
| 5g | $1520 | Check With Us |
: Cat #: V0576 CAS #: 790299-79-5 Purity ≥ 98%
Description: Masitinib (formerly also known as AB1010) is a novel, potent, orally bioavailable, selective and multi-targeted inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, it shows weak inhibition to ABL and c-Fms.
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| Molecular Weight (MW) | 498.64 |
|---|---|
| Molecular Formula | C28H30N6OS |
| CAS No. | 790299-79-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (200.5 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 4 mg/mL (8.0 mM) | |
| Solubility In Vivo | 4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 30mg/mL |
| SMILES Code | O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4 |
| Synonyms | AB-1010; AB 1010; AB1010; Masitinib. Brand name: Kinavet; Masivet. |
| Protocol | In Vitro | Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, masitinib demonstrates weak inhibition of Abl and c-Fms. Masitinib more strongly inhibits degranulation, cytokine production, and bone marrow mast cell migration than imatinib. 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. Masitinib inhibits Kit gain-of-function mutants, including V559D mutant and Δ27 mouse mutant with IC50 of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC50 of 10 and 30 nM, respectively. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0055 mL | 10.0273 mL | 20.0545 mL | 40.1091 mL |
| 5mM | 0.4011 mL | 2.0055 mL | 4.0109 mL | 8.0218 mL |
| 10mM | 0.2005 mL | 1.0027 mL | 2.0055 mL | 4.0109 mL |
| 20mM | 0.1003 mL | 0.5014 mL | 1.0027 mL | 2.0055 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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The dilution calculator equation
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.