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Ponatinib hydrochloride

Cat. No. M9009

All AbMole products are for research use only, cannot be used for human consumption.

Ponatinib hydrochloride Structure
Synonym:

AP24534 HCl

Size Price Availability Quantity
10mg USD 50 In stock
25mg USD 90 In stock
50mg USD 140 In stock
100mg USD 210 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 569.03
Formula C29H28ClF3N6O
CAS Number 1114544-31-8
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Gozgit JM, et al. Mol Cancer Ther. Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models.

[2] Gozgit JM, et al. Mol Cancer Ther. Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies.

[3] OHare T, et al. Cancer Cell. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

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

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