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Angiogenesis FGFR Ponatinib

Ponatinib

Catalog No. T2372   CAS 943319-70-8
Synonyms: AP24534

Ponatinib 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).

Ponatinib, CAS 943319-70-8
Pack Size Availability Price/USD Quantity
10 mg In stock 50.00
50 mg In stock 72.00
100 mg In stock 112.00
200 mg In stock 157.00
1 mL * 10 mM (in DMSO) In stock 50.00
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Purity 99.58%
Purity 99.00%
Purity 98.00%
Purity 99.57%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description Ponatinib 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).
Targets&IC50 Abl : ic50 0.37 nM (cell free) ,   c-Kit : ic50 12.5nM ,   c-Src : ic50 5.4 nM (cell free) ,   FGFR1 : ic50 2.2 nM (cell free) ,   PDGFRα : ic50 1.1 nM (cell free) ,   VEGFR2 : ic50 1.5 nM (cell free) ,   LYN : ic50 0.24 nM (cell free)
Kinase Assay 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].
Cell Research
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].
Cell lines: Ba/F3 cells expressing Bcr-Abl or a range of single mutations in the kinase domain of Bcr-Abl
Animal Research
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].
Animal Model: Mouse xenograft models of Ba/F3 cells expressing Bcr-Abl or Bcr-AblT315I
Synonyms AP24534
Purity 99.58%
Molecular Weight 532.56
Formula C29H27F3N6O
CAS No. 943319-70-8

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 53.3 mg/mL (100 mM)

Ethanol: 26.6 mg/mL (50 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 10 mg/mL

Citations

References and Literature
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.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Autophagy Compound Library Tyrosine kinase inhibitor library FDA-approved Drug Library Cytokine Inhibitor Library Kinase Inhibitor Library Fluorochemical Library Anti-Cardiovascular Disease Compound Library Angiogenesis related Compound Library

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