NVP-BSK805 dihydrochloride salt form · dihydrochloride · Parent NVP-BSK 805

NVP-BSK805 dihydrochloride 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

Data Sheet SDS COA

NVP-BSK805 dihydrochloride structure

CAS No.: 1942919-79-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 650.00	BP-02300A-250mg	In stock	Get quote
500 mg	USD 1,050.00	BP-02300A-500mg	In stock	Get quote
1 g	USD 1,650.00	BP-02300A-1g	In stock	Get quote
2 g	USD 1,650.00	BP-02300A-2g	In stock	Get quote
5 g	Inquire	BP-02300A-5g	In stock	Inquire
10 g	Inquire	BP-02300A-10g	In stock	Inquire

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Related forms

BP-02300 — NVP-BSK 805

Description

NVP-BSK805 dihydrochloride 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

NVP-BSK805 dihydrochloride is a potent and selective quinoxaline JAK2 inhibitor with IC50 values of 0.48, 0.56 and 0.58 nM for JAK2 JH1, FL JAK V617F and FL JAK2 wt respectively. Within the JAK family, NVP-BSK805 displays more than 20-fold selectivity towards JAK2 in vitro, as well as excellent selectivity in broader kinase profiling. The compound blunts constitutive STAT5 phosphorylation in JAK2(V617F)-bearing cells, with concomitant suppression of cell proliferation and induction of apoptosis. In vivo, NVP-BSK805 exhibited good oral bioavailability and a long half-life. The inhibitor was efficacious in suppressing leukemic cell spreading and splenomegaly in a Ba/F3 JAK2(V617F) cell-driven mouse mechanistic model. Furthermore, NVP-BSK805 potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.

Identifiers

SMILES: FC1=C(CN2CCOCC2)C(F)=CC(C3=C4N=C(C5=CN(C6CCNCC6)N=C5)C=NC4=CC=C3)=C1.Cl.Cl
InChIKey: NUOCAPALWRHKCU-UHFFFAOYSA-N

Specifications

MW (average): 563.4700
Formula: C₂₇H₃₀Cl₂F₂N₆O
CAS No.: 1942919-79-0
Physical state: Solid
Color: Light yellow 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 -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO,H2O

In vitro: DMSO : 50 mg/mL H2O : < 0.1 mg/mL

Documents

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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