MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)。

Imatinib Mesylate

CAS No. : 220127-57-1

MCE 國(guó)際站：Imatinib Mesylate

產(chǎn)品活性：Imatinib Mesylate (STI571 Mesylate) 是一種酪氨酸激酶抑制劑，可抑制 c-Kit，Bcr-Abl 和 PDGFR (IC₅₀=100 nM)。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶點(diǎn)：c-Kit  |  Bcr-Abl  |  PDGFR  |  Autophagy

In Vitro: Imatinib (STI571) Mesylate inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM. Imatinib (STI571) mesylate is very effective (in vitro IC₅₀ of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC₅₀, 410 nM) and PDGFR (in vitro IC₅₀, 380 nM). Imatinib (STI571) mesylate is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC₅₀ of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2. Imatinib mesylate selectively inhibits the activity of Bcr/Abl, c-Kit and PDGFR kinases. Imatinib mesylate reveals distinct and rapid antileukemic activity in chronic myelogenous leukemia (CML) and Philadelphia-positive (Ph⁺) acute lymphoblastic leukemia (ALL).

In Vivo: Animals treated with Imatinib Mesylate show a decrease of mean body weight throughout the whole study. Body weight loss is noticeable in mice from groups that receive chemotherapy and the vitamin D analog combined treatment. The body weight decrease of mice treat with both combined Imatinib mesylate and PRI-2191 is the highest (15%) on Day 22 of the experiment, but after that day, mice start to recover. In a rat Ischemia/reperfusion injury (IRI) model, Imatinib mesylate attenuates lung injury by an antipermeability and antiinflammatory effect. The delivery and function of Imatinib mesylate in the lung is also confirmed in this model.

相關(guān)產(chǎn)品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Antiviral Compound Library  |  CNS-Penetrant Compound Library  |  Autophagy Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  NMPA-Approved Drug Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Alzheimer's Disease Compound Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Therapy Drug Library   |  Anti-Parkinson's Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Angiogenesis-Related Compound Library  |  Anti-Liver Cancer Compound Library   |  Rare Diseases Drug Library  |  Children’s Drug Library  |  EMA-Approved Drug Library  |  FDA-Approved Anticancer Drug Library  |  Human Metabolite Library  |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Off-patent Drug Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Cytokine Inhibitors Library  |  Cell Death Library  |  SNIPER(ABL)-013  |  Sennoside B  |  AT9283  |  Bafetinib  |  Flumatinib mesylate  |  Multi-kinase-IN-2  |  PP58  |  c-Kit-IN-5-1  |  CT52923  |  Olverembatinib  |  Pexidartinib  |  ENMD-2076 Tartrate  |  GNF-2  |  AZD2932  |  Toceranib phosphate  |  BCR-ABL-IN-6  |  Ponatinib hydrochloride  |  GNF-5  |  Famitinib malate  |  AC710 Mesylate  |  Hypothemycin  |  Nintedanib  |  Motesanib Diphosphate  |  Vamotinib  |  Tandutinib  |  Telatinib mesylate  |  CT-721  |  Tyrphostin AG1433  |  Masitinib  |  Nintedanib-¹³C,d₃

熱門(mén)產(chǎn)品線：重組蛋白  |  化合物庫(kù)  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標(biāo)記物  |  寡核苷酸  |  抗體  |  點(diǎn)擊化學(xué)

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry