Vamotinib
Based on 1 Customer Validation
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. 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.
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- Pureté: 99.89%
- CAS No.: 1416241-23-0
- Formule: C29H27F3N6O
- Masse moléculaire:532.56
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 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)[2]
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Cell Line
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Type | Value | Description | References |
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| K562 | IC50 |
1 nM
Compound: PF-114
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Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
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[PMID: 35551036] |
Vamotinib (0-1 µM) inhibits ABL kinase and its mutants with IC50s of 0.49, 0.78, 1.0 µM for ABL, ABL(T315l), ABL(H396P), respectively[1].
Vamotinib (0-1000 nM) inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner[1].
Vamotinib (0-2000 nM) shows anti-proliferative activity in Ba/F3 cells expressing native BCR/ABL[1].
Vamotinib (0-100 nM) induces apoptosis in Ba/F3 cells expressing BCR/ABL and BCR/ABL-T315I[1].
Vamotinib (0-1000 nM) inhibits the growth of Ph+ patient-derived cell lines in k562, kcl-22, SupB15, Tom-1, BV-173 cells[1].
Vamotinib (0-1000 nM) suppresses growth of Ph+ PD-LTC with nonmutational resistance as well as T315I mutation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells
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Concentration:0, 10, 25, 50, 100, 500, 1000 nM
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Incubation Time:
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Result:Inhibited the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner and inhibited substrate phosphorylation as shown by the reduced Crkl-phosphorylation and downstream activation of Stat5 by BCR/ABL, as well as by BCR/ABL-T315I.
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Cell Line:Ba/F3 cells
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Concentration:0, 50, 500, 2000 nM
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Incubation Time:
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Result:Potently inhibited proliferation of Ba/F3 cells expressing native BCR/ABL in a dose-dependent manner and shows no effects on empty vector-transduced Ba/F3 cells in the presence of IL-3 (10 ng/ml).
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Cell Line:Ba/F3 cells
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Concentration:0-100 nM
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Incubation Time:
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Result:Induced apoptosis in Ba/F3 cells expressing BCR/ABL and BCR/ABL-T315I in a dose dependent manner.
Vamotinib (50 mg/kg; p.o.; once daily for 20 days) prolongs the survival of mice with both BCR/ABL- and BCR/ABL-T315I-driven CML-like disease[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/cAnNRj-Foxn1nu mice (K562 nude mouse xenograft model)[1]
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Dosage:25, 40 mg/kg
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Administration:Oral gavage; daily for 14 consecutive days
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Result:Caused a 100% reduction of the mean tumor volume within 4 weeks.
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Animal Model:8-12 weeks, C57BL/6N mice (CML-like disease mouse model)[1]
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Dosage:50 mg/kg
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Administration:P.o.; once daily for 20 days
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Result:Extended median survival significantly from 28 days to 39.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1416241-23-0
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Appearance Solid
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Masse moléculaire 532.56
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Formule C29H27F3N6O
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Color Off-white to light yellow
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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
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Synonyms
PF-114
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : 50 mg/mL (93.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.69 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8777 mL | 9.3886 mL | 18.7772 mL | 46.9431 mL |
| 5 mM | 0.3755 mL | 1.8777 mL | 3.7554 mL | 9.3886 mL | |
| 10 mM | 0.1878 mL | 0.9389 mL | 1.8777 mL | 4.6943 mL | |
| 15 mM | 0.1252 mL | 0.6259 mL | 1.2518 mL | 3.1295 mL | |
| 20 mM | 0.0939 mL | 0.4694 mL | 0.9389 mL | 2.3472 mL | |
| 25 mM | 0.0751 mL | 0.3755 mL | 0.7511 mL | 1.8777 mL | |
| 30 mM | 0.0626 mL | 0.3130 mL | 0.6259 mL | 1.5648 mL | |
| 40 mM | 0.0469 mL | 0.2347 mL | 0.4694 mL | 1.1736 mL | |
| 50 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.9389 mL | |
| 60 mM | 0.0313 mL | 0.1565 mL | 0.3130 mL | 0.7824 mL | |
| 80 mM | 0.0235 mL | 0.1174 mL | 0.2347 mL | 0.5868 mL |
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