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

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.

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

NVP-BSK805 Chemical Structure

NVP-BSK805 Chemical Structure

CAS No. : 1092499-93-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 173 In-stock
Solution
10 mM * 1 mL in DMSO USD 173 In-stock
Solid
1 mg USD 76 In-stock
5 mg USD 160 In-stock
10 mg USD 260 In-stock
25 mg USD 520 In-stock
50 mg USD 830 In-stock
100 mg USD 1330 In-stock
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NVP-BSK805:

NVP-BSK805 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE NVP-BSK805

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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[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 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NVP-BSK805 Related Antibodies
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].

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

490.55

Formula

C27H28F2N6O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (203.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0385 mL 10.1926 mL 20.3853 mL
5 mM 0.4077 mL 2.0385 mL 4.0771 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.89%

COA (252 KB) HNMR (285 KB) LCMS (95 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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0385 mL 10.1926 mL 20.3853 mL 50.9632 mL
5 mM 0.4077 mL 2.0385 mL 4.0771 mL 10.1926 mL
10 mM 0.2039 mL 1.0193 mL 2.0385 mL 5.0963 mL
15 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3975 mL
20 mM 0.1019 mL 0.5096 mL 1.0193 mL 2.5482 mL
25 mM 0.0815 mL 0.4077 mL 0.8154 mL 2.0385 mL
30 mM 0.0680 mL 0.3398 mL 0.6795 mL 1.6988 mL
40 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2741 mL
50 mM 0.0408 mL 0.2039 mL 0.4077 mL 1.0193 mL
60 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8494 mL
80 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
100 mM 0.0204 mL 0.1019 mL 0.2039 mL 0.5096 mL
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NVP-BSK805 Related Classifications

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.

Keywords:

NVP-BSK8051092499-93-8JAKJanus kinaseATP-competitiveJAK2JH1homologyJAK1JAK3TYK2Inhibitorinhibitorinhibit

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