Ponatinib

10mg

Cat. No.: 37-N29

$119.00

Ponatinib, also known as AP24534, is considered to be a pan-BCR-ABL inhibitor. It was specifically designed to bind BCR-ABL with very high potency and to inhibit the entire spectrum of mutants conferring resistance against other tyrosine kinase inhibitors (TKIs), such as VEGFR2, FGFR1, PDGFRα, mutant FLT3 phosporylation and LYN among others, including the T315I mutant that is resistant to all current therapies. It has been shown to suppress BCR-ALB(T315I)-driven tumor growth in mice.

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Details

TECHNICAL INFORMATION

Other Names: 3-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-benzamide

Chemical Formula: C29H27F3N6O

CAS Number: 943319-70-8

Molecular Weight: 532.56

Purity: >98%

IC50= 0.5 & 11 nM

Appearance: Pale Yellow Solid

Solubility: DMSO (100mM)

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO.

References

Zirm. E. | et al. (2012). Ponatinib may overcome resistance of FLT3-ITD harbouring additional point mutations | notably the previously refractory F691I mutation. BR J Haematol. 157:483-92.

Lierman. E. | et al. (2012). Ponatinib is active against imatinib-resistant mutants of FIP1L1-PDGFRA and KIT | and against FGFR1-derived fusion kinases. Leukemia. 26:1693-5.

Gozgit | J.M. | et al (2012). Ponatinib (AP24534) | a multitargeted pan-FGFR-amplified or mutated cancer models. Mol Cancer Ther. 11:690-9.

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