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^[1].

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.

534.60

C₂₈H₃₂F₂N₈O

1180158-99-9

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ringel F, et al. Effects of Jak2 type 1 inhibitors NVP-BSK805 and NVP-BVB808 on Jak2 mutation-positive and Bcr-Abl-positive cell lines. Acta Haematol. 2014;132(1):75-86.  [Content Brief]