NVP-BSK805
Based on 3 publication(s) in Google Scholar
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
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- Pureté: 99.30%
- CAS No.: 1092499-93-8
- Formule: C27H28F2N6O
- Masse moléculaire:490.55
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NVP-BSK805
More
Activité biologique
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JAK2 JH1 0.48 nM (IC50) |
FL JAK2 V617F 0.56 nM (IC50) |
FL JAK2 wt 0.58 nM (IC50) |
TYK2 JH1 10.76 nM (IC50) |
JAK3 JH1 18.68 nM (IC50) |
JAK1 JH1 31.63 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| SET-2 | GI50 |
88 nM
Compound: 26
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Growth inhibition of human SET2 cells expressing JAK2V617F mutant after 72 hrs by colorimetric WST1 assay
Growth inhibition of human SET2 cells expressing JAK2V617F mutant after 72 hrs by colorimetric WST1 assay
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[PMID: 20231096] |
NVP-BSK805 (BSK 805) is a JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. NVP-BSK805 inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC50s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 is ATP-competitive, with aclculated Ki of 0.43 ± 0.02 nM. NVP-BSK805 suppresses the growth of JAK2V617F-bearing acute myeloid leukemia cell lines with GI50 of <100 nM. NVP-BSK805 blocks the STAT5 phosphorylation at ≥100 nM concentrations, and shows a bias for JAK2 over JAK1 and JAK3 inhibition in the JAK2V617F-mutant cell lines[1].
NVP-BSK805 (5 μM) improves P-gp inhibitory activity. NVP-BSK805 increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1092499-93-8
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Appearance Solid
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Masse moléculaire 490.55
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Formule C27H28F2N6O
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Color Off-white to yellow
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SMILES
FC1=C(CN2CCOCC2)C(F)=CC(C3=C4N=C(C5=CN(C6CCNCC6)N=C5)C=NC4=CC=C3)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Pharmaceuticals (Basel)
Patchouli Alcohol Protects the Heart against Diabetes-Related Cardiomyopathy through the JAK2/STAT3 Signaling Pathway. [Abstract]2024 May 14;17(5):631. PMID: 38794201 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Solvant et solubilité
DMSO : 100 mg/mL (203.85 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. 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. 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)
Protocole
The antiproliferative activity of JAK2 inhibitors is determined by incubating cells for 72 hours (96 hours for MB-02 and MUTZ-8 cells) with an 8-point concentration range of NVP-BSK805 and cell proliferation relative to NVP-BSK805 is measured using the colorimetric WST-1 cell viability readout. Of each triplicate treatment, the mean is calculated and these data are plotted in XLfit 4 to determine the half-maximal growth inhibition (GI50) values[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Concomitantly with NVP-BSK805 treatment, female BALB/c mice receive daily s.c. injections (in 100 μL saline buffer) of 10 units of rhEpo for 4 consecutive days. Controls are injected corresponding volumes of saline buffer. Mice are sacrificed 24 hours after the final dose and total blood, spleen, and bone marrow are taken for further analysis. Animals are 8 to 10 weeks of age at treatment start (20-25 g body weight) and are kept under optimal hygienic conditions with free access to food and water[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55. [Content Brief]
[2]. Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0385 mL | 10.1926 mL | 20.3853 mL | 50.9632 mL |
| 5 mM | 0.4077 mL | 2.0385 mL | 4.0771 mL | 10.1926 mL | |
| 10 mM | 0.2039 mL | 1.0193 mL | 2.0385 mL | 5.0963 mL | |
| 15 mM | 0.1359 mL | 0.6795 mL | 1.3590 mL | 3.3975 mL | |
| 20 mM | 0.1019 mL | 0.5096 mL | 1.0193 mL | 2.5482 mL | |
| 25 mM | 0.0815 mL | 0.4077 mL | 0.8154 mL | 2.0385 mL | |
| 30 mM | 0.0680 mL | 0.3398 mL | 0.6795 mL | 1.6988 mL | |
| 40 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2741 mL | |
| 50 mM | 0.0408 mL | 0.2039 mL | 0.4077 mL | 1.0193 mL | |
| 60 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8494 mL | |
| 80 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6370 mL | |
| 100 mM | 0.0204 mL | 0.1019 mL | 0.2039 mL | 0.5096 mL |
NVP-BSK805 Related Classifications
HY-14722 Related Classifications
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