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Ponatinib

产品编号 T2372 CAS 943319-70-8

别名: 帕纳替尼, AP24534, 普纳替尼

Ponatinib (AP24534) 是一种有口服活性的多靶点激酶抑制剂，抑制Abl、PDGFRα、VEGFR2、FGFR1和Src 的IC50分别为 0.37 nM、1.1 nM、1.5 nM、2.2 nM 和 5.4 nM。

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Ponatinib, CAS 943319-70-8

规格	价格/CNY	货期
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 * 10 mM (in DMSO)	￥ 616	现货

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其他形式的 Ponatinib:

Ponatinib Hydrochloride
现货
Ponatinib-d8
询价

选择批次

纯度: 99.74%

纯度: 99.58%

纯度: 99.57%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
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	Ponatinib (AP24534) potently inhibited native ABL (IC50: 0.37 nM), ABL T315I (IC50: 2.0 nM), and other clinically important ABL kinase domain mutants (IC50: 0.30–0.44 nM). AP24534 also inhibited SRC (IC50: 5.4 nM) and members of the VEGFR, FGFR, and PDGFR families of receptor tyrosine kinases. AP24534 did not inhibit Aurora kinase family members, nor did it inhibit the insulin receptor or CDK2/Cyclin E. AP24534 potently inhibited proliferation of Ba/F3 cells expressing native BCR-ABL (IC50: 0.5 nM). All BCR-ABL mutants tested remained sensitive to AP24534 (IC50: 0.5–36 nM) including BCR-ABLT315I (IC50: 11 nM) [1]. Treatment with ponatinib efficiently inhibited the growth of CMPs expressing Hes1 with F/P, F/P-T674I, or F/P-D842V with an IC50 of 0.15 nM, 0.35 nM, or 1.71 nM, respectively. In accordance, ponatinib dose-dependently suppressed the activation of F/P and its downstream STAT5 and ERK in these cytokine-independent cells [2]. Ponatinib potently inhibits receptor phosphorylation and cellular proliferation with IC50 values comparable to those required for inhibition of BCR-ABL (0.3 to 20 nmol/L) [3].
体内活性	Daily oral treatment with 2.5 or 5 mg/kg AP24534 for 19 days prolonged median survival to 27.5 and 30 days, respectively. In a xenograft model of Ba/F3 BCR-ABLT315I cells, tumor growth was inhibited by AP24534 in a dose-dependent manner compared to vehicle-treated mice, with significant suppression of tumor growth upon daily oral dosing at 10 and 30 mg/kg. Daily oral dosing of 50 mg/kg AP24534 caused significant tumor regression, with a 96% reduction in mean tumor volume at the final measurement compared to the start of treatment [1]. Ponatinib (1–25 mg/kg, p.o.) was administered orally, once daily for 28 days, to mice bearing MV4-11 xenografts. ponatinib potently inhibited tumor growth in a dose-dependent manner. Administration of 1 mg/kg led to significant inhibition of tumor growth (TGI = 46%) and doses of 2.5 mg/kg or greater resulted in tumor regression. Dosing with 10 or 25 mg/kg led to complete and durable tumor regression [3].
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, AP24534, 普纳替尼
化合物与蛋白结合的复合物	FGFR1 in complex with ponatinib.
分子量	532.56
分子式	C29H27F3N6O
CAS No.	943319-70-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 26.6 mg/mL (50 mM)

DMSO: 53.3 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.8777 mL	9.3886 mL	18.7772 mL	46.9431 mL
	5 mM	0.3755 mL	1.8777 mL	3.7554 mL	9.3886 mL
	10 mM	0.1878 mL	0.9389 mL	1.8777 mL	4.6943 mL
	20 mM	0.0939 mL	0.4694 mL	0.9389 mL	2.3472 mL
	50 mM	0.0376 mL	0.1878 mL	0.3755 mL	0.9389 mL
DMSO	100 mM	0.0188 mL	0.0939 mL	0.1878 mL	0.4694 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. O'Hare T, et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell, 2009, 16(5), 401-412. 2. Uchida T, et al. Hes1 upregulation contributes to the development of FIP1L1-PDGRA-positive leukemia in blast crisis. Exp Hematol. 2014 May;42(5):369-379.e3. 3. Gozgit JM, et al. Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol Cancer Ther, 2011, 10(6), 1028-1035. 4. Lin H, Lu P, Zhou M, et al. Purification of recombinant human fibroblast growth factor 13 in E. coli and its molecular mechanism of mitogenesis[J]. Applied microbiology and biotechnology. 2019: 1-11.

文献引用

1. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866. 2. Lin H, Lu P, Zhou M, et al. Purification of recombinant human fibroblast growth factor 13 in E. coli and its molecular mechanism of mitogenesis. Applied Microbiology and Biotechnology. 2019: 1-11 3. Yan H, Wu W, Hu Y, et al.Regorafenib inhibits EphA2 phosphorylation and leads to liver damage via the ERK/MDM2/p53 axis.Nature Communications.2023, 14(1): 2756. 4. Oeller M, Jaksch-Bogensperger H, Templin M, et al.Transcription Factors STAT3 and MYC Are Key Players of Human Platelet Lysate-Induced Cell Proliferation.International Journal of Molecular Sciences.2022, 23(24): 15782.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：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 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ponatinib 943319-70-8 Angiogenesis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors VEGFR FGFR Bcr-Abl PDGFR Src c-Kit 帕纳替尼 Platelet-derived growth factor receptor orally inhibit multi-targeted VEGFR2 Fibroblast growth factor receptor Abl active AP 24534 Inhibitor AP-24534 PDGFRα kinase FGFR1 AP24534 Vascular endothelial growth factor receptor 普纳替尼 inhibitor

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Ponatinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords