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Ponatinib

产品编号 T2372Cas号 943319-70-8
别名 帕纳替尼, 普纳替尼, AP24534

Ponatinib (AP24534) 是一种有多靶点激酶抑制剂,具有口服活性,可以抑制 Abl、PDGFRα、VEGFR2、FGFR1 和 Src (IC50=0.37/1.1/1.5/2.2/5.4 nM)。Ponatinib 具有抗肿瘤活性,可以用于治疗成人慢性粒细胞白血病。

Ponatinib

Ponatinib

纯度: 99.74%
产品编号 T2372 别名 帕纳替尼, 普纳替尼, AP24534Cas号 943319-70-8

Ponatinib (AP24534) 是一种有多靶点激酶抑制剂,具有口服活性,可以抑制 Abl、PDGFRα、VEGFR2、FGFR1 和 Src (IC50=0.37/1.1/1.5/2.2/5.4 nM)。Ponatinib 具有抗肿瘤活性,可以用于治疗成人慢性粒细胞白血病。

规格价格库存数量
10 mg¥ 669现货
50 mg¥ 1,900现货
100 mg¥ 2,683现货
200 mg¥ 3,940现货
1 mL x 10 mM (in DMSO)¥ 616现货
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纯度:99.74%
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产品介绍

生物活性
产品描述
Ponatinib (AP24534) is a multi-targeted kinase inhibitor with oral activity that inhibits Abl, PDGFRα, VEGFR2, FGFR1, and Src (IC50=0.37/1.1/1.5/2.2/5.4 nM). Ponatinib has antitumor activity for the treatment of chronic granulocytic leukemia in adults. leukemia.
靶点活性
PDGFRα:1.1 nM (cell free), c-Src:5.4 nM (cell free), Abl:0.37 nM (cell free), FGFR1:2.2 nM (cell free), Lyn:0.24 nM (cell free), VEGFR2:1.5 nM (cell free)
体外活性
方法:亲本 Ba/F3 细胞和表达天然或突变 BCR-ABL Ba/F3 细胞的用 Ponatinib (0-10000 nM) 处理 72 h,使用 MTS assay 检测细胞活力。
结果:Ponatinib 有效地抑制表达天然 BCR-ABL 的 Ba/F3 细胞的增殖 (IC50=0.5 nM)。所有测试的 BCR-ABL 突变体对 Ponatinib 保持敏感 (IC50=0.5-36 nM),包括 BCR-ABLT315I (IC50=11 nM)。亲本 Ba/F3 细胞的生长仅在显著更高的 IC50 (1713 nM) 下受到抑制,表明对 BCR-ABL 阳性细胞的抑制具有显著的差异选择性。[1]
方法:AML 细胞系 MV4-11、Kasumi-1、KG1 和 EOL1 用 Ponatinib (0.03-100 nmol/L) 处理 1 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:Ponatinib 以剂量依赖的方式抑制所有 4 种 RTK (FLT3、KIT、FGFR1 和 PDGFRα) 的磷酸化,IC50 值在 0.3-20 nmol/L 之间。[2]
体内活性
方法:为测试体内抗肿瘤活性,将 Ponatinib (2.5-50 mg/kg in 0.5% CMC) 灌胃给药给注射 Ba/F3: BCR-ABLT315I 细胞的 SCID 小鼠,每天一次,持续十九天。
结果:Ponatinib 的治疗以剂量依赖的方式抑制肿瘤生长,延长了生存期。[1]
激酶实验
AP24534 was profiled against >100 kinases by Reaction Biology Corporation using the Kinase Hotspot assay, which utilizes 10 μM [33P]-ATP, recombinant kinase domain, peptide substrate, and a range of 10 concentrations of inhibitor to establish an IC50 value [1].
细胞实验
Ba/F3 cell lines were distributed in 96-well plates (4 × 10^3 cells/well) and incubated with escalating concentrations of AP24534 for 72 hr. The inhibitor ranges used were: 0–625 nM for cells expressing BCR-ABL and 0–10,000 nM for BCR-ABL negative cells. Proliferation was measured using an MTS-based viability assay. IC50 values are reported as the mean of three independent experiments performed in quadruplicate. For cell proliferation experiments with CML or normal primary cells, mononuclear cells were plated in 96-well plates (5 × 10^4 cells/well) over graded concentrations of AP24534 (0–1000 nM) in RPMI supplemented with 10% FBS, L-glutamine, penicillin/streptomycin, and 100 μM β-mercaptoethanol. Following a 72 hr incubation, cell viability was assessed by subjecting cells to an MTS assay. All values were normalized to the control wells with no drug [1].
动物实验
Briefly, tumor xenografts were established by the subcutaneous implantation of MV4-11 cells (1 × 10^7 in 50% Matrigel) into the right flank of female CB.17 severe combined immunodeficient mice and dosing was initiated when the average tumor volume reached approximately 200 mm^3. Ponatinib was formulated in aqueous 25 mmol/L citrate buffer (pH = 2.75) and mice were dosed orally once daily for 4 weeks. The tumors were measured in 2 dimensions (length and width) with a caliper in millimeters. Tumor volume (mm3) was calculated with the following formula: tumor volume = (length × width^2)/2. Tumor growth inhibition (TGI) was calculated as follows: TGI = (1 ? ΔT/ΔC) × 100, where ΔT stands for mean tumor volume change of each treatment group and ΔC for mean tumor volume change of control group. The tumor volume data were collected and analyzed with a 1-way ANOVA test to determine the overall difference among groups. Each ponatinib treatment group was further compared to the vehicle control group for statistical significance using Dunnett's Multiple Comparison Test. A P-value less than 0.05 was considered to be statistically significant and a P-value less than 0.01 to be highly statistically significant [3].
别名帕纳替尼, 普纳替尼, AP24534
化学信息
分子量532.56
分子式C29H27F3N6O
CAS No.943319-70-8
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 26.6 mg/mL (50 mM)
DMSO: 16.67 mg/mL (31.3 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5.33 mg/mL (10.01 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
溶液配制表
10% DMSO+40% PEG300+5% Tween 80+45% Saline/DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.8777 mL9.3886 mL18.7772 mL93.8861 mL
5 mM0.3755 mL1.8777 mL3.7554 mL18.7772 mL
10 mM0.1878 mL0.9389 mL1.8777 mL9.3886 mL
DMSO/Ethanol
1mg5mg10mg50mg
20 mM0.0939 mL0.4694 mL0.9389 mL4.6943 mL
Ethanol
1mg5mg10mg50mg
50 mM0.0376 mL0.1878 mL0.3755 mL1.8777 mL

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TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
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体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

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