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NVP-BSK805 2HCl (1092499-93-8(free base))

Catalog No. T6294 CAS T6294

Synonyms: NVP-BSK805 dihydrochloride, BSK 805, NVP-BSK805 (dihydrochloride)

NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.

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NVP-BSK805 2HCl (1092499-93-8(free base)) Chemical Structure

NVP-BSK805 2HCl (1092499-93-8(free base)), CAS T6294

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
2 mg	In stock	$ 95.00
5 mg	In stock	$ 177.00
10 mg	In stock	$ 245.00
25 mg	In stock	$ 455.00
50 mg	In stock	$ 642.00
100 mg	In stock	$ 919.00
500 mg	In stock	$ 1,860.00
1 mL * 10 mM (in DMSO)	In stock	$ 398.00

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Description	NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.
Targets&IC50	JAK2:0.5 nM
In vitro	NVP-BSK805 is found to potently inhibit JAK2, whereas displaying more than 20-fold selectivity towards JAK1, JAK3, and TYK2. NVP-BSK805 causes half-maximal inhibition of full-length JAK2V617F and JAK2 wild-type enzymes at 0.5 nM. NVP-BSK805 blocks the growth of JAK2V617F cells (Ba/F3) and induces apoptosis with a GI50 at concentrations ＜100 nM. As constitutive STAT5 phosphorylation in dependent on JAK2, NVP-BSK805 is found to potently suppress STAT5 phophorylation at ≥ 100 nM concentrations in the JAK2 V617F -mutant cell lines, like MB-02. Incubation of SET-2 cells with 150 nM and 1 μM of NVP-BSK805, which corresponds to concentration yielding 75% and 95% growth inhibition, respectively, for 24, 48, and 72 hours lead to concentration- and time- dependent induction of apoptosis. These results are evidenced by the detection of cleaved PARP, reduced Bcl-xL expression, and a strong increase in the number of cells with less than 2N DNA content. [1] NVP-BSK805 triggered cell death requires activation of caspase cascades and is overcome by caspase inhibition in both SET-2 and MB-02 cells. NVP-BSK805 modulates the post-translational modification of Bim and levels of Mcl-1 in JAK2V617F cells, SET-2 and MB-02 cells. [2]
In vivo	Oral bioavailability of NVP-BSK805 in mice is estimated to be 45%, while it is 50% in rats. Oral administration of NVP-BSK805 at 150 mg/kg suppresses STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell–driven mouse model. NVP-BSK805 suppresses rhEpo-induced STAT5 phosphorylation as well as rhEpo-mediated polycythemia and splenomegaly in BALB/c mice at doses of 25, 50, and 100 mg/kg orally. [1]
Cell Research	The anti-proliferative activity of JAK2 inhibitors is determined by incubating cells for 72 hours with an 8-point concentration range of compound and cell proliferation relative to DMSO-treated cells is measured using the colorimetric WST-1 (Roche Diagnostics GmbH) cell viability readout. Of each triplicate treatment, the mean is calculated and these data are plotted in XLfit 4 (ID Business Solutions, Ltd.) to determine the half-maximal growth inhibition (GI50) values.(Only for Reference)

Synonyms	NVP-BSK805 dihydrochloride, BSK 805, NVP-BSK805 (dihydrochloride)
Molecular Weight	563.47
Formula	C27H28F2N6O·2HCl
CAS No.	T6294

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 3 mg/mL (5.32 mM)

DMSO: 113 mg/mL (200.54 mM)

Ethanol: 15 mg/mL (26.62 mM)

References and Literature

1. Baffert F, et al. Mol Cancer Ther, 2010, 9(7), 1945-1955. 2. Rubert J, et al. BMC Cancer, 2011, Jan(19), 11-24.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Lung Cancer Compound Library Bioactive Compound Library Anti-Liver Cancer Compound Library Anti-Prostate Cancer Compound Library Angiogenesis related Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

NVP-BSK805 2HCl (1092499-93-8(free base)) T6294 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK NVP-BSK805 dihydrochloride NVP-BSK-805 Dihydrochloride BSK 805 NVP BSK805 2HCl (1092499 93 8(free base)) BSK805 NVP-BSK-805 NVPBSK805 2HCl (1092499938(free base)) NVP-BSK805 (dihydrochloride) NVP-BSK 805 Dihydrochloride NVP-BSK 805 NVP-BSK805 Dihydrochloride NVP-BSK805 2HCl (1092499-93-8 free base) NVP-BSK805 BSK-805 NVP-BSK-805 2HCl (1092499-93-8(free base)) inhibitor inhibit

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