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Ponatinib hydrochloride

Cat. No. M9009
Ponatinib hydrochloride Structure
Synonym:

AP24534 HCl

Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 240 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Ponatinib hydrochloride potently inhibits proliferation of Ba/F3 cells expressing native BCR-ABL (IC50 = 0.5 nM). Ponatinib hcl (AP24534) inhibits the in vitro kinase activity of FLT3, KIT, FGFR1, and PDGFRα with IC50 values of 13, 13, 2, and 1 nM, respectively. Ponatinib inhibits phosphorylation of all 4 RTKs in a dose-dependent manner, with IC50 values between 0.3 to 20 nM.

In vivo, in a mouse xenograft model of Ba/F3 cells expressing native Bcr-Abl, AP24534 (2.5 mg/kg and 5 mg/kg) prolongs mice median survival. In the xenograft model of Ba/F3 Bcr-AblT315I, Ponatinib hydrochloride (10 mg/kg–50 mg/kg) significantly suppresses tumor growth. AP24534 (30 mg/kg) decreases the phosphorylated Bcr-Abl and phosphorylated CrkL levels in the tumors.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 569.03
Formula C29H28ClF3N6O
CAS Number 1114544-31-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models.
Gozgit JM, et al. Mol Cancer Ther. 2012 Mar;11(3):690-9. PMID: 22238366.

Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies.
Gozgit JM, et al. Mol Cancer Ther. 2011 Jun;10(6):1028-35. PMID: 21482694.

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.
OHare T, et al. Cancer Cell. 2009 Nov 6;16(5):401-12. PMID: 19878872.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ponatinib hydrochloride, AP24534 HCl supplier, Src-bcr-Abl, inhibitors

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