Dasatinib monohydrate

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Chemical Structure| 863127-77-9 同义名 : 达沙替尼一水合物 ;BMS-354825 monohydrate; Dasatinib(monohydrate)
CAS号 : 863127-77-9
货号 : A210354
分子式 : C22H28ClN7O3S
纯度 : 98%
分子量 : 506.02
MDL号 : MFCD08704581
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

2% DMSO+30% PEG 300+dd water 5 mg/mL

生物活性
靶点

  • c-Kit

    c-Kit (wt), IC50:79 nM

    c-Kit (D816V), IC50:37 nM

  • Src

    Src, IC50:0.8 nM

  • Src

    Src, IC50:0.8 nM

  • Abl

    Abl , IC50:0.6 nM
描述 Dasatinib monohydrate, also known as BMS-354825 monohydrate, is an orally active, ATP-competitive dual Src/Bcr-Abl inhibitor with potent antitumor properties. It has Ki values of 16 pM for Src and 30 pM for Bcr-Abl. The IC50 values for inhibiting Bcr-Abl and Src are less than 1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate exhibits significant activity against a range of targets including Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK, with IC50 values of less than 1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively. It shows antiproliferative effects on K562 chronic myelogenous leukemia (CML), PC3 human prostate cancer, MDA-MB-231 human breast cancer, and WiDr human colon cancer cell lines, with IC50 values of less than 1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy in cells[1].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02883049 B Acute Lymphoblastic Leukemia... 展开 >> Central Nervous System Leukemia Ph-Like Acute Lymphoblastic Leukemia Testicular Leukemia Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia 收起 << Phase 3 Recruiting - -
NCT00390793 Acute Lymphoblastic Leukemia ... 展开 >> BCR-ABL1 Fusion Protein Expression Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive Philadelphia Chromosome Positive Recurrent Acute Lymphoblastic Leukemia t(9;22) 收起 << Phase 2 Active, not recruiting August 31, 2020 United States, Texas ... 展开 >> M D Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT02143414 Acute Lymphoblastic Leukemia ... 展开 >> B Acute Lymphoblastic Leukemia B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative Philadelphia Chromosome Positive Recurrent Adult Acute Lymphoblastic Leukemia Refractory Adult Acute Lymphoblastic Leukemia Untreated Adult Acute Lymphoblastic Leukemia 收起 << Phase 2 Recruiting - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.88mL

1.98mL

0.99mL

19.76mL

3.95mL

1.98mL
参考文献

[1]Dargart JL, Fish K, et al. Dasatinib therapy results in decreased B cell proliferation, splenomegaly, and tumor growth in a murine model of lymphoma expressing Myc and Epstein-Barr virus LMP2A. Antiviral Res. 2012 Jul;95(1):49-56.

[2]Shah NP, Lee FY, et al. Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood. 2006 Jul 1;108(1):286-91.