NVP-BVB808
NVP-BVB808 is a selective and ATP-competitive JAK2 inhibitor with an IC50 of 0.35 nM. NVP-BVB808 binds to JAK2’s ATP-binding site, stabilizes JAK2’s active conformation, increases JAK2 activation loop phosphorylation, and blocks downstream kinase function. NVP-BVB808 exhibits antiproliferative and pro-apoptosis effects, suppresses constitutive STAT5a phosphorylation. NVP-BVB808 can be used for the research of cancer, such as leukemia.
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- No. CAS: 1180158-99-9
- Fòrmula: C28H32F2N8O
- Peso molecular:534.60
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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JAK2 0.35 nM (IC50) |
STAT5 |
NVP-BVB808 (11 individual concentrations; 72 h) potently inhibits proliferation of JAK2-mutant CHRF-288-11, SET-2, and UKE-1 cells with GI50 values of 0.15 μM, 0.25 μM, and 0.22 μM respectively after 72 hours, shows weaker activity against HEL cells (GI50 = 2.13 μM), and inhibits proliferation of BCR-ABL-positive and JAK2 wild-type cell lines only at higher concentrations (GI50 = 0.73-3.20 μM)[1].
NVP-BVB808 (72 h) induces apoptosis in CHRF-288-11, SET-2, HEL, Lama-87, KU-812, BV173, K562, and KCL-22 cells, with the highest potency against CHRF-288-11 cells (IC50 = 0.3 μM) and decreasing potency across the remaining cell lines[1].
NVP-BVB808 (0-1 μM; 30 min) potently inhibits STAT5a phosphorylation in JAK2-mutant SET-2, and HEL cells at concentrations as low as 0.05 μM after 30 minutes, while showing minimal effect on BCR-ABL-positive K562 and KCL-22 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JAK2-mutant cell lines: CHRF-288-11, SET-2, HEL; BCR-ABL-positive cell lines: K562, KCL-22
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Concentration:0, 0.01, 0.05, 0.1, 0.5, 1 μM
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Incubation Time:30 min
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Result:Suppressed constitutive STAT5a phosphorylation in SET-2 cells at 0.1 μM.
Suppressed constitutive STAT5a phosphorylation in HEL cells at ~0.5 μM.
Showed only weak to no inhibition of STAT5a phosphorylation in BCR-ABL-positive K562 and KCL-22 cells at tested concentrations.
Chemical Information
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No. CAS 1180158-99-9
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Peso molecular 534.60
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Fòrmula C28H32F2N8O
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SMILES
FC(C=C1N2C3=NC(NC4=CN=C(N5C[C@H](N[C@H](C5)C)C)C=C4)=NC=C3C=C2)=C(C(F)=C1)CN6CCOCC6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NVP-BVB808 Related Classifications
HY-182430 Related Classifications
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