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

SKU: orb1300895

Description

NVP-BSK805 2HCl (1092499-93-8 free base) is a potent, ATP-competitive JAK2 inhibitor with an IC50 of 0.5 nM, demonstrating >20-fold selectivity over JAK1, JAK3, and TYK2. It is widely used in research to investigate JAK2-dependent signaling in cellular assays and hematological malignancy models.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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MW	563.47
Purity	97.41% (May vary between batches)
Formula	C₂₇H₂₈F₂N₆O·2HCl
SMILES	Cl.Cl.Fc1cc(cc(F)c1CN1CCOCC1)-c1cccc2ncc(nc12)-c1cnn(c1)C1CCNCC1
Target	Tyrosine Kinases,JAK
Solubility	Ethanol:15 mg/mL (26.62 mM);H2O:3 mg/mL (5.32 mM);DMSO:113 mg/mL (200.54 mM)

Bioactivity

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Target IC50	JAK2:0.5 nM
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. Read more...
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. 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. Read more...
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) Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Tyrosine Kinases, TyrosineKinases, Tyk2, BSK 805, BSK805, BSK-805, NVP BSK805 2HCl (1092499 93 8(free base)), NVP-BSK 805, NVP-BSK 805 Dihydrochloride, NVP-BSK805, NVP-BSK-805, NVP-BSK805 (dihydrochloride), NVPBSK805 2HCl (1092499938(free base)), NVP-BSK-805 2HCl (1092499-93-8(free base)), NVP-BSK805 2HCl (1092499-93-8(free base)), NVP-BSK805 dihydrochloride, NVP-BSK805 Dihydrochloride, NVP-BSK-805 Dihydrochloride, NVP-BSK805 2HCl (1092499-93-8 free base), JAK3, JAK2, JAK1

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID

57339395 ↗

Key Properties

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No computed properties available.

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