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Masitinib (AB1010)

Pharmacological effects Biological activity In vitro In vivo Feature
Masitinib (AB1010)
Masitinib (AB1010) structure
CAS No.
790299-79-5
Chemical Name:
Masitinib (AB1010)
Synonyms
Ab1010;Ab 1010;Ab-1010;Masivet;Mastinib;Masatinib;MASITINIB;masitinib API;asitinib (AB1010);Masitinib(AB1010)
CBNumber:
CB41509122
Molecular Formula:
C28H30N6OS
Formula Weight:
498.64
MOL File:
790299-79-5.mol

Masitinib (AB1010) Properties

Melting point:
90-95?C
storage temp. 
Refrigerator

SAFETY

Masitinib (AB1010) price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 13105 Masitinib ≥98% 790299-79-5 10mg $55 2018-11-19 Buy
Cayman Chemical 13105 Masitinib ≥98% 790299-79-5 25mg $131 2018-11-19 Buy
Cayman Chemical 13105 Masitinib ≥98% 790299-79-5 50mg $248 2018-11-19 Buy
Cayman Chemical 13105 Masitinib ≥98% 790299-79-5 100mg $468 2018-11-19 Buy

Masitinib (AB1010) Chemical Properties,Uses,Production

Pharmacological effects

Masitinib, also known as methotrexate masitinib, is studied and developed by the AB Science, a platelet-derived growth factor alpha/beta receptor tyrosine kinase inhibitor for the treatment of multiple myeloma, gastrointestinal stromal tumors and prostate cancer.
The drug had respectively, been entitled by FDA for the treatment of pancreatic cancer and ALS orphans disease in 2009 and 2015. On August 8, 2016, it has qualified as EMA orphan drug.
Masitinib is a novel kind of oral administrated tyrosine kinase inhibitors that could be targeted to immunizing important cellular mast cells and macrophages by inhibiting a certain amount of kinase. Based on its unique mechanism of action, masitinib can be developed for application in tumors, inflammatory diseases and certain central nervous system diseases.
In the oncology, due to its immunotherapy effect, Masitinib may affect the survival period of cancer patients (single administration or in combination with chemotherapy). By acting on mast cells and microglia, and further inhibiting the activation of the inflammatory process, Masitinib is effective against certain inflammatory, central nervous system disorders as well as symptoms associated with degeneration of these diseases.

Biological activity

Masitinib (AB1010) is a novel Kit and PDGFRα/β inhibitor with IC50 of 200 nM and 540 nM/800 nM, respectively, however with weak inhibits on ABL and c-Fms. Phase 3.

In vitro

Masitinib, at a concentration of ≤ 500 nM, it is a kind of ATP competitive inhibitors. Masitinib can also effectively inhibit the recombinant PDGFR and intracellular kinase Lyn, and FGFR3. However, Masitinib has a weak inhibitory effect on ABL and c-Fms. Masitinib acts on de-granulation, cytokine production, and bone marrow mast cell migration with the inhibitory effect being much stronger than imatinib. In Ba/F3 cells expressing human wild-type KIT, Masitinib can inhibit the SCF (stem cell factor)-induced cell proliferation with an IC50 being 150 nM and an IC50 value of being larger than 10 μM when inhibiting the IL-3 stimulated proliferation. In Ba/F3 cells expressing PDGFR-α, Masitinib is capable of inhibiting the PDGF-BB stimulated proliferation and PDGFR-alpha tyrosine phosphorylation with an IC50 of 300 nM. Masitinib acts on mast cell tumor cell lines and BMMC, and also inhibits the stimulated phosphorylation of human KIT tyrosine. Masitinib takes effect on the Ba/F3 cells to suppress the KIT-acquired functional mutations which include V559D mutations and Δ27 mutations with IC50s of 3 and 5 nM, respectively. Masitinib inhibits the cell proliferation of mast cell tumor cell lines including HMC-1α155 and FMA3 cells with the IC50 of 10 and 30 nM, respectively. Masitinib acts on two new ISS cell lines, inhibits cell growth and phosphorylation of PDGFR, indicating that Masitinib inhibits primary and metastatic ISS cell lines and is helpful in the clinical management of ISS.

In vivo

30 mg/kg Masitinib, when acting on the Ba/F3 transplanted tumor model expressing Δ27, is capable of inhibiting tumor growth and improving the survival time of the culture medium, and is non-toxic to both the heart and the gene. Daily oral administration of 12.5 mg/kg Masitinib improves all TTP (the grown tumor with the time). When the Masitinib and gemcitabine are used in combination to fight against the proliferation of the anti-gemcitabine cell lines during Mia Paca2 and Panc1 proliferation, they exhibit synergetic effects.

Feature

Masitinib has a better safety than other tyrosine inhibitors.

Chemical Properties

Off-White to Pale Yellow Solid

Uses

Masitinib is a novel tyrosine kinases inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, resectively.

Uses

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 2/3

Uses

Masitinib controlled-release implant for treating solid neoplasm.

Definition

ChEBI: A member of the class of benzamides that is the carboxamide resulting from the formal condensation of the carboxy group of 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid with the primary amino group of 4-methyl-N3-[4 (pyridin-3-yl)-1,3-thiazol-2-yl]benzene-1,3-diamine. It is a highly selective oral tyrosine kinase inhibitor.

Masitinib (AB1010) Preparation Products And Raw materials

Raw materials

Preparation Products


Masitinib (AB1010) Suppliers

Global( 139)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24192 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 27142 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 955 58
Shenzhen Nexconn Pharmatechs Ltd
15013857715
admin@nexconn.com CHINA 3193 58
GIHI CHEMICALS CO.,LIMITED
08657186217390
sales@gihichemicals.com CHINA 308 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 sales@jushengtech.com CHINA 28237 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Shanghai Yudiao Chemistry Technology Co.,Ltd Tel# +86 (21)37285211; Mb# 18964703211; QQ# 122752498 Skype# Yudiaochem
info@yudiaochem.com;122752498@qq.com China 273 58
shanghai aokchem co., ltd 021-68712331 QQ39130253
18621350903 aokchem@gmail.com China 333 58
Shanghai Scientia Pharmaceutical Technology Co., Ltd. 400-036-1573 / +86 (21) 54301573 / 61721573
+86 (21) 51861981 sales@scientiapharm.com,scientiapharm@gmail.com China 254 62

View Lastest Price from Masitinib (AB1010) manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-12-24 Masitinib (AB1010)
790299-79-5
US $2.00 / kg 1kg 99% 100kg career henan chemical co

790299-79-5(Masitinib (AB1010))Related Search:


  • asitinib (AB1010)
  • MASITINIB
  • 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide
  • 4-((4-Methylpiperazin-1-yl)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)-1,3-thiazol-2-yl)amino)phenyl)benzamide
  • Ab 1010
  • Ab1010
  • Ab-1010
  • Mastinib
  • Masitinib(AB1010)
  • 4-(4-Methyl-piperazin-1-ylMethyl)-N-[4-Methyl-3-(4-pyridin-3-yl-thiazol-2-ylaMino)-phenyl]-benzaMide
  • Masatinib
  • Masivet
  • MASITINIB 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[4-Methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]aMino]phenyl]benzaMide
  • N-(4-Methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benz
  • 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide Masitinib (AB1010)
  • masitinib API
  • N-(4-Methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)b
  • Masatinib (AB1010, Masivet)
  • 790299-79-5
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Sulfur & Selenium Compounds
  • Anti-cancer&immunity
  • Inhibitors
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