NVP-BSK805 is an ATP-competitiveJAK2inhibitor, withIC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM forJAK2JH1 (JAK homology 1),JAK1JH1,JAK3JH1, andTYK2JH1, respectively^[1].

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 K_iof 0.43 ± 0.02 nM. NVP-BSK805 suppresses the growth of JAK2^V617F-bearing acute myeloid leukemia cell lines with GI₅₀of<100 nm. nvp-bsk805 blocks the stat5 phosphorylation at ≥100 nm concentrations, and shows a bias for jak2 over jak1 jak3 inhibition in jak2^V617F-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].

NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2^V617Fcell-driven mouse model^[1].
NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice^[1].

490.55

Solid

C₂₇H₂₈F₂N₆O

1092499-93-8

Room temperature in continental US; may vary elsewhere.

DMSO : 125 mg/mL(254.82 mM;Need ultrasonic)

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