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Imatinib mesylate Produkt Beschreibung

CAS-Nr.220127-57-1
Bezeichnung:
Englisch Name:Imatinib mesylate
Synonyma:
GLIVEC;GLEEVEC;Gleevac;STI-571;CGP54148B;CGP 57148;CGP-57148B;Genfatinib;220127-57-1;tinib Mesylate
CBNumber:CB7173646
Summenformel:C30H35N7O4S
Molgewicht:589.71
MOL-Datei:220127-57-1.mol
Imatinib mesylate physikalisch-chemischer Eigenschaften
Schmelzpunkt:: 214-224°C
storage temp. : -20°C Freezer
Löslichkeit: H2O: soluble10mg/mL, clear
Aggregatzustand: White solid
Farbe: white to beige
InChIKey: YLMAHDNUQAMNNX-UHFFFAOYSA-N
CAS Datenbank: 220127-57-1(CAS DataBase Reference)
Sicherheit
Kennzeichnung gefährlicher: Xn
R-Sätze:: 22
WGK Germany : 3
RTECS-Nr.: CV5520550
HS Code : 29350090
Giftige Stoffe Daten: 220127-57-1(Hazardous Substances Data)

Imatinib mesylate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
Off-White Solid
Originator
Novartis (Switzerland)
Verwenden
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)
Verwenden
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
Verwenden
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.
Verwenden
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.
Trademarks
Gleevec, Glivec
Allgemeine Beschreibung
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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Imatinib mesylate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.      Global( 396)Lieferanten     
Firmenname Telefon Fax E-Mail Land Produktkatalog Edge Rate
Jinan Jianfeng Chemical Co., Ltd
15562555968
info@pharmachemm.com CHINA 615 58
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105sales@frappschem.com China 886 50
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95sales@capotchem.com China 19918 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925Abel@chembj.com CHINA 3203 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21954 58
Chengdu Henghui Pharm Tec Co. Ltd.
13540674322 15828370308,QQ:2879822141
028-89481236service@2hpharm.com CHINA 121 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497sales01@cooperate-pharm.com CHINA 1530 55
Hebei Jiangkai Trading Co., Ltd
0086-17197824289/17197824028
alice@hbjkai.com CHINA 274 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693info@tianfuchem.com CHINA 20680 55
Shanghai Time Chemicals CO., Ltd.
+86-021-57951555
+86-021-57951555jack.li@time-chemicals.com CHINA 1367 55
 
220127-57-1(Imatinib mesylate)Verwandte Suche:
Methyl-4-hydroxybenzoat Bensulfuron methyl Imatinib Kresoxim-methyl Methyl Brommethan 2-Pyridylamin Methylacrylat Thiophanat-methyl 3-Pyridylamin Gatifloxacin mesylate Pazufloxacin mesilate 3-Carboxy-1-ethyl-6-fluor-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxochinolinmonomethansulfonat Methylacetat N,N-Dimethylpyridin-4-amin Parathion-methyl (ISO)
Imatinib for system suitability Imatinib mesylate / 4-[(4-Methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[[4-(3-pyridyl)pyrimidin-2-yl]amino]phenyl]benzamide Gleevec (Imatinib) IMatinib Mesylate(STI-571) Imantinib mesylate 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[4-Methyl-3-[[4-(3-pyridinyl)-2-pyriMidinyl]aMino]phenyl]benzaMide Methanesulfonate GLIVEC GLEEVEC IMATINIB METHANESULFONATE CGP-57148B 4-[(4-methylpiperazin-1-yl)methyl]-n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate Bcr-abl Inhibitor IV, Imatinib - CAS 220127-57-1 - Calbiochem Gleevac Gleevec (IMatinib Mesylate) CGP54148B 4-(4-Methylpiperazin-1-ylMethyl)-N-[4-Methyl-3-(4-pyridin-3-yl-pyriMidin-2-ylaMino)phenyl]benzaMide Methanesulfonic acid salt N-(4-Methyl-3-((4-(pyridin-3-yl)pyriMidin-2-yl)aMino)phenyl)-4-(4-Methylpiperazin-1-yl)benzaMide Methanesulfonate tinib Mesylate Gleevec, Glivec, CGP-57148B, STI-571 4-[(4-methyl-1-piperazinyl)methyl]-n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate STI-571 IMATINIB BASE(IMA-3) ImatinibMesylate/Gleevec Imatinib Methanesulfonate, STI-571, CGP-57148B, Glivec, IMATINIB MESYLATE (IMATINIB METHANESULFONATE) alpha-IMATINIB MESYLATE Imatinib mesylate(TINIBS ) - 220127-57-1 221027-57-1 C30H35N7O4S Intermediates & Fine Chemicals Pharmaceuticals Tyrosine Kinase Inhibitors Aromatics Heterocycles API Glivec, CGP-57148B, STI-571 C29H31N7OCH4O3S C29H31N7OCH4SO3 152549-95-5 Imatinib mesylate Imatinib Methanesulphonate Salt N-(4-Methyl-3-((4-(pyridin-3-yl)pyriMidin-2-yl)aMino)phenyl)-4-((4-Methylpiperazin-1-yl)Methyl)benzaMide Methanesulfonate N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonic acid ST-1571 Mesylate Imatinib mesylate 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate 4-[(4-Methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide mesylate CGP 57148 Genfatinib 220127-57-1 Imatinib mesylate, >=99% 4-(4-methylpiperazinomethyl)benzoyl chloride dihydrochloride 4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)phenyl]benz Bcr-abl Inhibitor IV, Imatinib Imatinib mesylate(alpha Form) Imatinib Mesylate 220127-57-1
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