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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;GLEEVEC;Gleevac;STI-571;CGP54148B;CGP 57148;CGP-57148B;Genfatinib;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. 
-20°C Freezer
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)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn
Risk Statements  22
WGK Germany  3
RTECS  CV5520550
HS Code  29350090
Hazardous Substances Data 220127-57-1(Hazardous Substances Data)
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
Precautionary statements:

Imatinib mesylate price More Price(12)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1027 Imatinib mesylate ≥98% (HPLC) 220127-57-1 10mg $33.8 2018-11-13 Buy
Sigma-Aldrich SML1027 Imatinib mesylate ≥98% (HPLC) 220127-57-1 100mg $115 2018-11-13 Buy
TCI Chemical I0936 Imatinib Mesylate >98.0%(HPLC) 220127-57-1 100mg $37 2018-11-22 Buy
TCI Chemical I0936 Imatinib Mesylate >98.0%(HPLC) 220127-57-1 1g $220 2018-11-22 Buy
Cayman Chemical 13139 Imatinib (mesylate) ≥98% 220127-57-1 25mg $25 2018-11-13 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( 392)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Jinan Jianfeng Chemical Co., Ltd
15562555968
info@pharmachemm.com CHINA 617 58
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 887 50
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3217 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
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Chengdu Henghui Pharm Tec Co. Ltd.
13540674322 15828370308,QQ:2879822141
028-89481236 service@2hpharm.com CHINA 121 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
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+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
Hebei Jiangkai Trading Co., Ltd
0086-17197824289/17197824028
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Henan Tianfu Chemical Co.,Ltd.
0371-55170693
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Shanghai Time Chemicals CO., Ltd.
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View Lastest Price from Imatinib mesylate manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-12-18 Imatinib mesylate
220127-57-1
US $7.00 / kg 1kg 99% 100kg career henan chemical co
2018-08-20 Imatinib mesylate
220127-57-1
US $1.00 / KG 1G 98% 100KG career henan chemical co
2018-07-26 Imatinib mesylate
220127-57-1
US $100.00 / KG 1KG 99% Customized career henan chemical co

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