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  • 普纳替尼|T2372|TargetMol

普纳替尼|T2372|TargetMol

Ponatinib
943319-70-8
￥669 10mg 起订
￥1900 50mg 起订
￥2683 100mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
普纳替尼
英文名称：
Ponatinib
CAS号：
943319-70-8
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.74%
产品类别：
抑制剂
货号：
T2372

Product Introduction

Bioactivity

名称Ponatinib
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.
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].
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].
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].
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]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度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.
关键字Src | Ponatinib | Platelet-derived growth factor receptor | Bcr-Abl | orally | inhibit | multi-targeted | VEGFR2 | Fibroblast growth factor receptor | Abl | VEGFR | active | PDGFR | AP 24534 | FGFR | Inhibitor | AP-24534 | PDGFRα | kinase | FGFR1 | Autophagy | Vascular endothelial growth factor receptor
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普纳替尼|||帕纳替尼|||AP24534|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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