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普纳替尼 Ponatinib

Product Name: 普纳替尼 Ponatinib

Description: Ponatinib is an orally bioavailable multitargeted receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor AP24534 inhibits unmutated and all mutated forms of Bcr-Abl, including T315I, the highly drug therapy-resistant missense mutation of Bcr-Abl. This agent also inhibits other tyrosine kinases including those associated with vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs); in addition, it inhibits the tyrosine kinase receptor TIE2 and FMS-related tyrosine kinase receptor-3 (Flt3).

Name: Ponatinib
CAS#: 943319-70-8 (free base)
Chemical Formula: C29H27F3N6O
Exact Mass: 532.21984
Molecular Weight: 532.56
Elemental Analysis: C, 65.40; H, 5.11; F, 10.70; N, 15.78; O, 3.00

Synonym: AP24534; AP-24534; AP 24534; Ponatinib. Brand name: Iclusig.

IUPAC/Chemical Name: 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide.

InChi Key: PHXJVRSECIGDHY-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H27F3N6O/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39)

SMILES Code: O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN=C5C=CC=NN54)=C3

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Ponatinib free base is soluble in DMSO at 50 mg/mL; soluble in ethanol at 25 mg/mL with warming; very poorly soluble in water. The solubility of ponatinib in pH 1.7, 2.7, and 7.5 buffers is 7790 mcg/ml, 3.44 mcg/ml, and 0.16 mcg/ml, respectively, indicating a decrease in solubility with increasing pH.

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 – 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001