Dasatinib达沙替尼一水合物,863127-77-9

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Dasatinib monohydrate

CAS No. : 863127-77-9

MCE 国际站：Dasatinib monohydrate

产品活性：Dasatinib (BMS-354825) monohydrate 是一种具有口服活性的，ATP 竞争性的，双重 Src/Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 K_i 值分别为 16 pM 和 30 pM。Dasatinib monohydrate 抑制 Bcr-Abl 和 Src 的IC₅₀ 分别为 <1.0 nM 和 0.5 nM。Dasatinib monohydrate 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy  |  Apoptosis

作用靶点：Bcr-Abl  |  Src  |  Autophagy  |  Apoptosis

In Vitro: Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC₅₀s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively.
Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC₅₀s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively.

In Vivo: Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels.
Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t_1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (F_po) in this study is 27%.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound 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  |  Anti-Parkinson's Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Angiogenesis-Related 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  |  Non-steroidal Anti-Inflammatory Compound Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Off-patent Drug Library  |  Membrane Protein-targeted Compound Library  |  Cell Death Library  |  MG-132  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  LY294002  |  Tamoxifen  |  Paclitaxel  |  Y-27632  |  Acetylcysteine  |  Angiotensin II human  |  2-Deoxy-D-glucose  |  Staurosporine  |  SB-431542  |  Actinomycin D  |  Deferoxamine mesylate  |  Bortezomib  |  5-Fluorouracil  |  Trametinib  |  Sorafenib  |  Oxaliplatin  |  Gemcitabine  |  Temozolomide  |  Rotenone  |  Mdivi-1  |  Elesclomol  |  Ruxolitinib  |  Decitabine  |  SP600125  |  MK-2206 dihydrochloride  |  Etoposide  |  Monomethyl auristatin E

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds