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Vamotinib

CAT: 0804-HY-147414-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-147414-01Size:5 mg
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Description
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABLT315I), 9.5 nM (ABLE255K), 2.0 nM (ABLF317I), 7.4 nM (ABLG250E), 1.0 nM (ABLH396P), 2.8 nM (ABLM351T), 12 nM (ABLQ252H), and 4.1 nM (ABLY253F), respectively[1][2]. Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CAS Number
1416241-23-0
Product Name Alternative
PF-114
UNSPSC
12352005
Target
Bcr-Abl
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/vamotinib.html
Purity
99.89
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
O=C(C1=CC=C(C)C(C#CC2=NN=C3C=CC=CN23)=C1)NC4=CC=C(CN5CCN(CC5)C)C(C(F)(F)F)=C4
Molecular Formula
C29H27F3N6O
Molecular Weight
532.56
References & Citations
[1]Mian AA, et al. PF-114, a potent and selective inhibitor of native and mutated BCR/ABL is active against Philadelphia chromosome-positive (Ph+) leukemias harboring the T315I mutation. Leukemia. 2015 May;29 (5) :1104-14.|[2]Ivanova ES, et al. PF‑114, a novel selective inhibitor of BCR‑ABL tyrosine kinase, is a potent inducer of apoptosis in chronic myelogenous leukemia cells. Int J Oncol. 2019 Jul;55 (1) :289-297.|[3]Mian AA, et al. PF-114, a potent and selective inhibitor of native and mutated BCR/ABL is active against Philadelphia chromosome-positive (Ph+) leukemias harboring the T315I mutation. Leukemia. 2015 May;29 (5) :1104-14.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture and light)
Scientific Category
Reference compound1
Clinical Information
Phase 2

Alternative Products

CatalogName
GTR19184877-01Vamotinib

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