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Imatinib mesylate

a small-molecule inhibitor
Imatinib mesylate
Imatinib mesylate structure
CAS No.
220127-57-1
Chemical Name:
Imatinib mesylate
Synonyms
GLIVEC;STI-571;GLEEVEC;Gleevac;CGP 57148;CGP54148B;Genfatinib;CGP-57148B;220127-57-1;tinib Mesylate
CBNumber:
CB7173646
Molecular Formula:
C30H35N7O4S
Formula Weight:
589.71
MOL File:
220127-57-1.mol

Imatinib mesylate Properties

Melting point:
214-224°C
storage temp. 
2-8°C
solubility 
H2O: soluble10mg/mL, clear
form 
White solid
color 
white to beige
InChIKey
YLMAHDNUQAMNNX-UHFFFAOYSA-N
CAS DataBase Reference
220127-57-1(CAS DataBase Reference)
FDA UNII
8A1O1M485B
NCI Dictionary of Cancer Terms
Gleevec; imatinib mesylate; STI571
NCI Drug Dictionary
Gleevec
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P301+P312+P330
Hazard Codes  Xn
Risk Statements  22
WGK Germany  3
RTECS  CV5520550
HS Code  29350090

Imatinib mesylate price More Price(14)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1027 Imatinib mesylate ≥98% (HPLC) 220127-57-1 10mg $36.4 2021-03-22 Buy
Sigma-Aldrich SML1027 Imatinib mesylate ≥98% (HPLC) 220127-57-1 100mg $124 2021-03-22 Buy
Sigma-Aldrich 5.04595 Bcr-abl Inhibitor IV, Imatinib - CAS 220127-57-1 - Calbiochem 220127-57-1 50 mg $129 2021-03-22 Buy
Sigma-Aldrich Y0001692 Imatinib for system suitability European Pharmacopoeia (EP) Reference Standard 220127-57-1 $190 2021-03-22 Buy
TCI Chemical I0936 Imatinib Mesylate >98.0%(HPLC) 220127-57-1 100mg $46 2021-03-22 Buy

Imatinib mesylate Chemical Properties,Uses,Production

a small-molecule inhibitor

Imatinib mesylate (also called Gleevec) is a small-molecule inhibitor of the fusion protein Bcr-Abl, the causal agent in chronic myelogenous leukemia.
As an inhibitor of PDGFR, imatinib mesylate appears to have utility in the treatment of a variety of dermatological diseases. Imatinib has been reported to be an effective treatment for FIP1L1-PDGFRalpha+ mast cell disease, hypereosinophilic syndrome, and dermatofibrosarcoma protuberans.

Description

In May 2001, the FDA approved imatinib as a new cancer drug after a record review time of just 2.5 months. Imatinib was launched as Gleevec in the US for chronic myelogenous leukemia (CML) in blast crisis, accelerated phase or chronic phase after interferon-alpha failure. This compound can be prepared by a four step sequence from a condensation of the 1-(3-pyridyl)ethanone with dimethyl formamide dimethylacetal, followed by successive cyclization with the methyl-nitrophenyl guanidine, hydrogenolysis and condensation with the benzoyl chloride of the methylpiperazine. Imatinib is the first of a new class of anticancer drugs that are specifically designed to target the molecular pathways involved (oncogenic event) in the development of disease. The Brc-Abl oncoprotein is a constitutively active tyrosine kinase that causes CML. Imatinib is a competitive inhibitor of this tyrosine kinase as well as Abl, Kit and the PDGFR kinases It binds to the ATP-binding site of the target kinase and prevents the transfer of phosphate from ATP to the tyrosine residues of various substrates and consequently blocks the proliferation of the leukemic cells. Phase II studies demonstrated that in chronic phase CML, over 90% of the patients had their leukocyte counts return to normal and 56% had a major cytogenic response. No phase III data is currently available. It is clear from the evidence available that imatinib has advantages over IFN-alpha, such as reduced toxicity, more rapid hematological response, higher rate of cytogenic response and oral administration. The drug is well tolerated, producing few side effects, classified as grade 1 nausea, muscle cramps, diarrhea, edema and vomiting. Imatinib is metabolized primarily by the CYP3A4 enzyme system and drugs capable of modulating this system would be expected to modify the patient's exposure. Novartis expects to launch imatinib for the treatment of gastrointestinal stromal tumors in 2002.

Chemical Properties

Off-White Solid

Originator

Novartis (Switzerland)

Uses

A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL)

Uses

Imatinib Mesylate is orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. Imatinib also known as Gleevec, Glivec, CGP-57148B, STI-571 & Imatinib

Uses

Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.

Uses

echinocandin antifungal, active against infections with Aspergillus and Candida, inhibits cell wall synthesis

Definition

ChEBI: A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.

brand name

Gleevec, Glivec

General Description

Imatinib is available in 100- and 400-mg capsules for oraladministration and is indicated for the treatment of CML,gastrointestinal stromal tumors (GIST) that express Kit andacute lymphoplastic leukemia that is positive for thePhiladelphia chromosome.
Bioavailability of the agent is nearly 100% by the oralroute. The agent is highly protein bound and metabolized tothe N-desmethyl derivative by CYP3A4-mediated removalof the piperazinyl methyl group. The resulting metabolite issimilar to the parent in activity. Elimination occurs primarilyin the feces, and the terminal half-life is 18 hours forthe parent and 40 hours of the N-desmethyl metabolite.Resistant forms of the TK are known, which have alteredamino acids that prevent binding. In addition, there may beincreased levels of the kinase itself. The drug is also a substratefor Pgp and an additional efflux transporter known asbreast cancer resistance protein (BCRP), both of which removethe drug from the cell. These transporters are also inhibitedby the agent as well. Severe side effects include ascites,neutropenia, thrombocytopenia, skin rash, andpulmonary edema. Less serious side effects include nausea/vomiting, heartburn, and headache but overall, the agentis better tolerated than most other medications used in treatingthe disease.

Imatinib mesylate Preparation Products And Raw materials

Raw materials

Preparation Products


Imatinib mesylate Suppliers

Global( 525)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 886 50
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Shanghai Time Chemicals CO., Ltd.
+8618017249410 +86-021-57951555
+86-021-57951555 jack.li@time-chemicals.com CHINA 1365 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8909 55
Guangzhou PI PI Biotech Inc
+8618371201331
020-81716319 sales@pipitech.com;87478684@qq.com China 3245 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3013 60
Shanghai Yingrui Biopharma Co., Ltd.
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View Lastest Price from Imatinib mesylate manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-12-01 Imatinib Mesylate
220127-57-1
US $19.10 / KG 1KG 99% 10 ton Hebei Crovell Biotech Co Ltd
2021-11-30 Imatinib mesylate
220127-57-1
US $665.00 / Kg/Bag 1KG 99% 1T Baoji Guokang Bio-Technology Co., Ltd.
2021-11-15 Imatinib mesylate
220127-57-1
US $0.00 / KG 1KG 99% 200000pcs Hebei Yirun Sega Biological Technology Co. Ltd

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