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Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR/ABL and BCR/ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $108 | In Stock | |
5 mg | $272 | In Stock | |
10 mg | $446 | In Stock | |
25 mg | $796 | In Stock | |
50 mg | $1,090 | In Stock | |
100 mg | $1,490 | In Stock | |
200 mg | $1,980 | In Stock | |
1 mL x 10 mM (in DMSO) | $319 | In Stock |
Description | Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR/ABL and BCR/ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease. |
Targets&IC50 | Abl (T315I):0.78 nM, Abl (H396P):1.0 nM, Abl (Y253F):4.1 nM, Abl (Q252H):12 nM, Abl (E255K):9.5 nM, Abl (F317I):2.0 nM, BCR-ABL:0.49 nM, Abl (G250E):7.4 nM |
In vitro | Vamotinib (0-1000 nM) inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner. Additionally, it can suppress the growth of Ph+ patient-derived cell lines, including K562, KCL-22, SupB15, Tom-1, BV-173, as well as Ph+ PD-LTC cells with non-mutated resistance and T315I mutation[1]. |
In vivo | In female BALB/cAnNRj-Foxn1nu mice (K562 nude mouse xenograft model), Vamotinib (25/40 mg/kg, oral gavage; 14 days) resulted in a 100% reduction in average tumor volume within 4 weeks. |
Alias | PF-114 |
Molecular Weight | 532.56 |
Formula | C29H27F3N6O |
Cas No. | 1416241-23-0 |
Smiles | CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3nnc4ccccn34)cc2C(F)(F)F)CC1 |
Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (56.33 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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