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Imatinib mesylate

Imatinib mesylate Struktur
220127-57-1
CAS-Nr.
220127-57-1
Englisch Name:
Imatinib mesylate
Synonyma:
GLEEVEC;GLIVEC;Imatinib (Glivec);Gleevac;STI-571;CGP54148B;CGP 57148;CGP-57148B;Genfatinib;tinib Mesylate
CBNumber:
CB7173646
Summenformel:
C30H35N7O4S
Molgewicht:
589.71
MOL-Datei:
220127-57-1.mol

Imatinib mesylate Eigenschaften

Schmelzpunkt:
214-224°C
storage temp. 
2-8°C
L?slichkeit
H2O: soluble10mg/mL, clear
Aggregatzustand
White solid
Farbe
white to beige
Stabilit?t:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
InChIKey
YLMAHDNUQAMNNX-UHFFFAOYSA-N
SMILES
C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)(=O)C1=CC=C(CN2CCN(C)CC2)C=C1.CS(O)(=O)=O
CAS Datenbank
220127-57-1(CAS DataBase Reference)

Sicherheit

Kennzeichnung gef?hrlicher Xn
R-S?tze: 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

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

Definition

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

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 H?ndler.

Global( 764)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hebei Mojin Biotechnology Co., Ltd
+86 13288715578 +8613288715578
sales@hbmojin.com China 12825 58
Hebei Chuanghai Biotechnology Co,.LTD
+86-13131129325
sales1@chuanghaibio.com China 5893 58
Sinoway Industrial co., ltd.
0592-5800732; +8613806035118
xie@china-sinoway.com China 988 58
shandong perfect biotechnology co.ltd
+86-53169958659; +8618596095638
sales@sdperfect.com China 294 58
Henan Bao Enluo International TradeCo.,LTD
+86-17331933971 +86-17331933971
deasea125996@gmail.com China 2472 58
Nanjing Fred Technology Co., Ltd
+86-25-84696168 +86-15380713688
Austin@fredbio.com China 2428 58
Henan Fengda Chemical Co., Ltd
+86-371-86557731 +86-13613820652
info@fdachem.com China 20288 58
Shaanxi TNJONE Pharmaceutical Co., Ltd
+8618092446649
sarah@tnjone.com China 1143 58
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
sales@frappschem.com China 880 50
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29791 60

220127-57-1()Verwandte Suche:


  • 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[[4-(3-pyridyl)pyrimidin-2-yl]amino]phenyl]benzamide
  • Imatinib mesylate / 4-[(4-Methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate
  • Gleevec (Imatinib)
  • IMatinib Mesylate(STI-571)
  • Gleevec, Glivec, CGP-57148B, STI-571
  • 4-[(4-Methyl-1-piperazinyl)Methyl]-N-[4-Methyl-3-[[4-(3-pyridinyl)-2-pyriMidinyl]aMino]phenyl]benzaMide Methanesulfonate
  • IMATINIB METHANESULFONATE
  • CGP-57148B
  • 4-[(4-methylpiperazin-1-yl)methyl]-n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate
  • Gleevac
  • Gleevec (IMatinib Mesylate)
  • CGP54148B
  • CGP54148B; STI571; GLEEVEC;GLIVEC
  • 4-(4-Methylpiperazin-1-ylMethyl)-N-[4-Methyl-3-(4-pyridin-3-yl-pyriMidin-2-ylaMino)phenyl]benzaMide Methanesulfonic acid salt
  • Imantinib mesylate
  • N-(4-Methyl-3-((4-(pyridin-3-yl)pyriMidin-2-yl)aMino)phenyl)-4-(4-Methylpiperazin-1-yl)benzaMide Methanesulfonate
  • tinib Mesylate
  • 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 )
  • 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
  • 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
  • GLIVEC; CGP-57148B; STI-571
  • Imatinib mesylate (Gleevec, Glivec, CGP-57148B, STI-571)
  • Imatinib for system suitability
  • Bcr-abl Inhibitor IV, Imatinib - CAS 220127-57-1 - Calbiochem
  • Imatinib for system suitability CRS
  • Imatinib mesilate CRS
  • Imatinib mesylate salt
  • ImatinibMesylate>
  • Imatinib Mesylate β form
  • Imatinib mesyL
  • Imatinib mesylate(API)
  • Imatinib mesylate USP/EP/BP
  • PIRARUBICIN /CAS-220127-57-1
  • Imatinib mesilate (Y0001691)
  • Imatinib MesylateQ: What is Imatinib Mesylate Q: What is the CAS Number of Imatinib Mesylate Q: What is the storage condition of Imatinib Mesylate Q: What are the applications of Imatinib Mesylate
  • Imatinib for system suitability (Y0001692)
  • 4-[(4-methyl-1-piperazinyl)methyl]-n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate
  • Imatinib mesylate(alpha Form)
  • Imatinib (STI-571) Mesylate
  • Imatinib Mesylate 220127-57-1
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