NVP-BSK 805 free base · Synonyms: NVP-BSK805

NVP-BSK805 is an ATP-competitive JAK2 inhibitor.

For research use only. Not for human or veterinary use.

Target JAK

Research area Cancer

Purity >98% Stock Inquire

NVP-BSK 805 structure

CAS No.: 1092499-93-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 550.00	BP-02300-250mg	In stock	Get quote
500 mg	USD 880.00	BP-02300-500mg	In stock	Get quote
1 g	USD 1,400.00	BP-02300-1g	In stock	Get quote
2 g	USD 2,250.00	BP-02300-2g	In stock	Get quote
3 g	USD 2,700.00	BP-02300-3g	In stock	Get quote
5 g	USD 3,600.00	BP-02300-5g	In stock	Get quote
10 g	Inquire	BP-02300-10g	In stock	Inquire

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Related forms

BP-02300A — NVP-BSK805 dihydrochloride

Description

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

Biological activity

In Vitro 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]. In Vivo NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-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].

Identifiers

SMILES: FC1=CC(=CC(F)=C1CN1CCOCC1)C1=C2N=C(C=NC2=CC=C1)C1=CN(N=C1)C1CCNCC1
InChIKey: IBPVXAOOVUAOKJ-UHFFFAOYSA-N

Specifications

MW (average): 490.5476
Formula: C₂₇H₂₈F₂N₆O
CAS No.: 1092499-93-8
Physical state: Solid
Color: off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

CoA On request
Handling Instructions

References

[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.

[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.

Same target

Search JAK

Same research area

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