Size | Price | |
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100mg | ||
250mg | ||
500mg |
ln Vitro |
With IC50 values 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 triHClide (BSK 805) is a JAK2 inhibitor. ..Full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F exhibit inhibited activity when exposed to NVP-BSK805 triHClide, with IC50 values of 0.58 ± 0.03 and 0.56 ± 0.04 nM, respectively. NVP-BSK805 trihydrochloride has a cumulative Ki of 0.43 ± 0.02 nM, making it ATP competitive. Acute myeloid leukemia cell lines containing JAK2V617F are inhibited in growth by NVP-BSK805 triHClide, with a GI50 <100 nM. At concentrations ≥100 nM, NVP-BSK805 triHClide inhibits STAT5 phosphorylation and, in the JAK2V617F mutant cell line, inhibits JAK2 more than JAK1 and JAK3. The P-gp inhibitory activity is increased by NVP-BSK805 triHClide (5 μM). Drug-resistant KBV20C cancer cells can be made more sensitive to VIC treatment by NVP-BSK805 triHClide at a dose of 10 μM, which is more effective than a dose of 5 μM [2].
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ln Vivo |
NVP-BSK805 triHClide (BSK 805; 150 mg/kg, oral) suppresses STAT5 phosphorylation, splenomegaly, and leukemic cell dissemination in a Ba/F3 JAK2V617F cell-driven animal model [1]. NVP-BSK805 triHClide (50, 75 and 100 mg/kg, orally) similarly suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice [1].
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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]. [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. |
Molecular Formula |
C27H31CL3F2N6O
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Molecular Weight |
599.93
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CAS # |
2320258-95-3
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Related CAS # |
NVP-BSK805;1092499-93-8;NVP-BSK805 dihydrochloride;1942919-79-0
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SMILES |
C1=CC2=NC=C(C3C=NN(C=3)C3CCNCC3)N=C2C(C2=CC(F)=C(C(F)=C2)CN2CCOCC2)=C1.Cl.Cl.Cl
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6669 mL | 8.3343 mL | 16.6686 mL | |
5 mM | 0.3334 mL | 1.6669 mL | 3.3337 mL | |
10 mM | 0.1667 mL | 0.8334 mL | 1.6669 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.