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Vamotinib
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.
Catalog No. T63746Cas No. 1416241-23-0
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Vamotinib
Catalog No. T63746Cas No. 1416241-23-0
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $133 | In Stock | |
| 2 mg | $196 | In Stock | |
| 5 mg | $328 | In Stock | |
| 10 mg | $538 | In Stock | |
| 25 mg | $1,080 | In Stock | |
| 50 mg | $1,730 | In Stock | |
| 100 mg | $2,780 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $388 | In Stock |
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CitedProduct Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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 (F317I):2.0 nM, Abl (T315I):0.78 nM, Abl (Y253F):4.1 nM, Abl (E255K):9.5 nM, BCR-ABL:0.49 nM, Abl (G250E):7.4 nM, Abl (H396P):1.0 nM, Abl (Q252H):12 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 |
| 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. | ||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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