2. Epigenetics
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  3. JAK
  4. NVP-BSK805 dihydrochloride

NVP-BSK805 dihydrochloride 

Cat. No.: HY-14722A Purity: 99.81%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

NVP-BSK805 dihydrochloride Chemical Structure

NVP-BSK805 dihydrochloride Chemical Structure

CAS No. : 1942919-79-0

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Solution
10 mM * 1 mL in DMSO USD 229 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 229 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 185 In-stock
Estimated Time of Arrival: December 31
10 mg USD 277 In-stock
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1254 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NVP-BSK805 dihydrochloride:

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1 Publications Citing Use of MCE NVP-BSK805 dihydrochloride

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JAK1 JAK2 JAK3 Tyk2 JAK

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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[1].

IC50 & Target[1]

JAK2 JH1

0.48 nM (IC50)

FL JAK2 V617F

0.56 nM (IC50)

FL JAK2 wt

0.58 nM (IC50)

TYK2 JH1

10.76 nM (IC50)

JAK3 JH1

18.68 nM (IC50)

JAK1 JH1

31.63 nM (IC50)

In Vitro

NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) 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 dihydrochloride (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

NVP-BSK805 (BSK805 dihydrochloride; 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

563.47

Appearance

Solid

Formula

C27H30Cl2F2N6O
CAS No.
SMILES

FC1=C(CN2CCOCC2)C(F)=CC(C3=C4N=C(C5=CN(C6CCNCC6)N=C5)C=NC4=CC=C3)=C1.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (88.74 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7747 mL 8.8736 mL 17.7472 mL
5 mM 0.3549 mL 1.7747 mL 3.5494 mL
10 mM 0.1775 mL 0.8874 mL 1.7747 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.81%

COA (254 KB) HNMR (133 KB) RP-HPLC (137 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

The antiproliferative activity of JAK2 inhibitors is determined by incubating cells for 72 hours (96 hours for MB-02 and MUTZ-8 cells) with an 8-point concentration range of NVP-BSK805 and cell proliferation relative to NVP-BSK805 is measured using the colorimetric WST-1 cell viability readout. Of each triplicate treatment, the mean is calculated and these data are plotted in XLfit 4 to determine the half-maximal growth inhibition (GI50) values[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Concomitantly with NVP-BSK805 treatment, female BALB/c mice receive daily s.c. injections (in 100 μL saline buffer) of 10 units of rhEpo for 4 consecutive days. Controls are injected corresponding volumes of saline buffer. Mice are sacrificed 24 hours after the final dose and total blood, spleen, and bone marrow are taken for further analysis. Animals are 8 to 10 weeks of age at treatment start (20-25 g body weight) and are kept under optimal hygienic conditions with free access to food and water[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

NVP-BSK8051942919-79-0JAKJanus kinaseATP-competitiveJAK2JH1homologyJAK1JAK3TYK2Inhibitorinhibitorinhibit

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