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790299-79-5 (Masitinib)

1

Identification

Masitinib Masitinib
Name Masitinib
Formula C28H30N6OS
MW 498.64
CAS No. 790299-79-5
EINECS
Smiles O=C(NC1=CC=C(C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4
Synonyms AB1010; Masivet; AB-1010; AB 1010; N-(4-methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
InChI InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32)
2

Introduction

Masitinib(AB-1010) is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. IC50 value: 200 nM (Kit); 540 nM/800 nM(PDGFRα/β) [1] Target: c-Kit; PDGFRα/β in vitro: 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.

Background Information

A potent, orally available protein tyrosine kinase inhibitor targeting c-Kit, PDGFR and FGFR3 ......by AOBIOUS INC
Masitinib (AB1010) is a tyrosine kinase inhibitor targeting stem cell factor receptor (c-kit) and platelet-derived growth factor (PDGF) receptor. It can enhance the antiproliferative effects of gemcitabine (GEM) in human pancreatic cancer cells. It potently inhibited human and murine KIT with activating mutations in the juxtamembrane domain. In vivo, masitinib (AB1010) blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant. Masitinib, a c-kit and PDGF-receptor tyrosine kinase inhibitor, may represent an innovative avenue of treatment in corticosteroid-dependent asthma. ......by AbMole BioScience
Masitinib (AB1010) is a protein tyrosine kinase inhibitor. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Masitinib is an orally bioavailable and multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity. ......by BOC Sciences
Cell-permeable. A protein tyrosine kinase (PTK) inhibitor. targeting KIT that is active, orally bioavailable in vivo, and has low toxicity. Masitinib also potently inhibited recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. In contrast, masitinib demonstrated weak inhibition of ABL and c-Fms and was inactive against a variety of other tyrosine and serine/threonine kinases. ......by BioVision, Inc.,
Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, and has weak inhibition to ABL and c-Fms. ......by MedChemexpress Co., Ltd.
Masitinib, also known as AB1010, is an orally bioavailable and multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity. Masitinib selectively binds to and inhibits both the wild-type and mutated forms of the stem cell factor receptor (c-Kit; SCFR); platelet-derived growth factor receptor (PDGFR); fibroblast growth factor receptor 3 (FGFR3); and, to a lesser extent, focal adhesion kinase (FAK). As a consequence, tumor cell proliferation may be inhibited in cancer cell types that overexpress these receptor tyrosine kinases (RTKs). Masitinib was approved for veterinary use. ......by MedKoo Biosciences, Inc.
A potent tyrosine kinase inhibitor targeting c-Kit and PDGFR with IC50 of 0.15 and 0.05 uM in cell based assays; also inhibits Lyn, and to a lesser extent, FGFR3, and inhibits KIT gain-of-function mutants V559D (IC50=3.0 nM) and Δ27 mouse mutant (IC50=5 nM); dose-dependently inhibits SCF-induced cell proliferation in Ba/F3 cells expressing human wild-type KIT (IC50=150 nM); inhibits tumour growth in vivo.Prostate cancerPhase 3 Clinical ......by ProbeChem
Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. ......by Selleck Chemicals LLC
Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines Ba/F3 cells expressing wild-type or mutant human Kit, HMC1, HMC-1α155
Conditions 0.1 nM - 10 μM; 48 hours
Method For the assay of Ba/F3 cell proliferation, microtitre plates are seeded with a total of 104 cells/well in 100 μL of RPMI 1640 medium with 10% foetal bovine serum at 37 °C. These are supplemented, or not, with either 0.1% conditioned medium from X63-IL-3 cells or 250 ng/mL murine SCF. The murine SCF, which activates Kit, is purified from the conditioned medium of SCF-producing CHO cells. Cells are grown for 48 hours at 37 °C with Masitinib and then incubated with 10 μL/well of WST-1 reagent for 3 hours at 37 °C. The amount of formazan dye formed is quantified by its absorbance at 450 nm using a scanning multiwell spectrophotometer. A blank well without cells is used as a background control for the spectrophotometer.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Ba/F3 Δ27 tumour model in female MBRI Nu/Nu mice
Dosage 30 mg/kg (intraperitoneal) or 10, 30, or 45 mg/kg (orally).
Formulation DMSO
Administration Intraperitoneal or orally administered.
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000029032

Storage condition

Store at or below -20 oC. by LC Laboratoies

Solubility

Soluble in DMSO at 200 mg/mL; very poorly soluble in ethanol or water; maximum solubility in plain water is estimated to be about 10-20 μM; buffers, serum, or other additives may increase or decrease the aqueous solubility. by LC Laboratoies
DMSO ≥95mg/mL Water <1.2mg/mL Ethanol ≥3.6mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 100 mg/mL (200.54 mM); Ethanol4 mg/mL (8.02 mM); Water<1 mg/mL (<1 mM); In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O30mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Masitinib AB Science SA Alzheimers disease 2012/1/31 2016/12/31 Phase 3 Clinical
Masitinib AB Science SA Gastrointestinal stromal tumor 2012/4/30 2015/12/31 Phase 3 Clinical
Masitinib AB Science SA Multiple myeloma 2011/5/31 2014/12/31 Phase 3 Clinical
Masitinib AB Science SA Asthma 2011/6/30 2015/12/31 Phase 3 Clinical
Masitinib AB Science SA Stage IV melanoma 2011/1/31 Phase 3 Clinical
Masitinib - Pre-registration
Masitinib - Phase 3
7

Safety Data of Masitinib

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
AbMole BioScience USA
Adipogen Corporation USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
BOC Sciences
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD60();50mg/USD108() USA
Cayman Chemical Company USA
LC Laboratoies 10mg/USD37(In stock);25mg/USD72(In stock);50mg/USD112(In stock);100mg/USD169(In stock);200mg/USD213(In stock);300mg/USD267(In stock);500mg/USD410(In stock);1g/USD538(In stock);2g/USD924(In stock) USA
MedChemexpress Co., Ltd. 10mg/USD60();50mg/USD108() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Pure Chemistry Scientific Inc. 5mg/USD75(In stock) USA
Selleck Chemicals LLC 10mM/1mLIn DMSO/USD82(In stock);10mg/USD90(In stock);25mg/USD170(In stock);200mg/USD870(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD60();50mg/USD108() China
Shanghai SPE Chemicals Co., Ltd. China
Target Molecule Corp. 2mg/USD27();5mg/USD43();10mg/USD77();25mg/USD138();50mg/USD248() USA
10

Related Products

Other Forms of 790299-79-5

Name CAS No Formula MW
Masitinib (mesylate) 1048007-93-7 C29H34N6O4S2 594.75

Recommended Compounds in PDGFR c-Kit

Name CAS No Formula MW
BIBF 1202 894783-71-2 C30H31N5O4 525.6
Masitinib (mesylate) 1048007-93-7 C29H34N6O4S2 594.75
Imatinib (hydrochloride) 862366-25-4 C29H32ClN7O 530.06
Flumatinib (mesylate) 895519-91-2 C30H33F3N8O4S 658.69
Flumatinib 895519-90-1 C29H29F3N8O 562.5887
SKLB610 1125780-41-7 C21H16F3N3O3 415.37
AZD2932 883986-34-3 C24H25N5O4 447.4864
Toceranib (phosphate) 874819-74-6 C22H28FN4O6P 494.45
Sunitinib 557795-19-4 C22H27FN4O2 398.47
AC710 1351522-04-7 C31H42N6O4 562.7
TAK-593 1005780-62-0 C23H23N7O3 445.47
Imatinib (Mesylate) 220127-57-1 C30H35N7O4S 589.7084
JI-101 900573-88-8 C22H20BrN5O2 466.33
ABT-348 1227939-82-3 C25H21FN6O2S 488.54
BIBF 1120 (esylate) 656247-18-6 C33H39N5O7S 649.7571
N-Desethyl Sunitinib 356068-97-8 C20H23FN4O2 370.42
Telatinib 332012-40-5 C20H16ClN5O3 409.8257
Sorafenib 284461-73-0 C21H16ClF3N4O3 464.83
SU14813 (maleate) 849643-15-8 C27H31FN4O8 558.56
Crenolanib 670220-88-9 C26H29N5O2 443.54

Recommended Compounds in Same Indication

Name CAS No Formula MW
Lu AE58054 467459-31-0 C20H19F5N2O 398.37
EVP-6124 550999-75-2 C16H17ClN2OS 320.84
Regorafenib 755037-03-7 C21H15ClF4N4O3 482.82
Trametinib 871700-17-3 C26H23FIN5O4 615.39
Quisinostat 875320-29-9 C21H26N6O2 394.4702
AT9283 896466-04-9 C19H23N7O2 381.43
IDO5L 914471-09-3 C9H7ClFN5O2 271.6356
MLN9708 1239908-20-3 C20H23BCl2N2O9 517.12
Panobinostat 404950-80-7 C21H23N3O2 349.43
SB-590885 405554-55-4 C27H27N5O2 453.54
SCH 527123 473727-83-2 C21H23N3O5 397.42
Beclometasone dipropionate 5534-09-8 C28H37ClO7 521.04
Tideglusib 865854-05-3 C19H14N2O2S 334.39
Setipiprant 866460-33-5 C24H19FN2O3 402.42
Linsitinib 867160-71-2 C26H23N5O 421.49
Carfilzomib 868540-17-4 C40H57N5O7 719.91
Levalbuterol (tartrate) 661464-94-4 C30H48N2O12 628.71
Cilostazol 73963-72-1 C20H27N5O2 369.46
AT13387 912999-49-6 C24H31N3O3 409.52
ARRY-520 (R enantiomer) 885060-08-2 C20H22F2N4O2S 420.48
11

Route of Synthesis

12

References

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More Information

Masitinib

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