NVP-BSK805 2HCl (BSK-805)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1340 | Check With Us |
| 500mg | $1950 | Check With Us |
| 1g | $2925 | Check With Us |
: Cat #: V0336 CAS #: 1942919-79-0 (2HCl) Purity ≥ 98%
Description: NVP-BSK805 2HCl (BSK805), the dihydrochloride salt of NVP-BSK805, is a novel, potent, selective and ATP-competitive JAK2 (Janus kinase) inhibitor with potential antitumor activity.
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| Molecular Weight (MW) | 563.47 |
|---|---|
| Molecular Formula | C27H28F2N6O.2HCl |
| CAS No. | 1942919-79-0 (2HCl) |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 113 mg/mL (200.5 mM)r |
| Water: 3 mg/mL (5.3 mM)r | |
| Ethanol: 15 mg/mL (26.6 mM) | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL |
| SMILES Code | FC1=C(CN2CCOCC2)C(F)=CC(C3=C4N=C(C5=CN(C6CCNCC6)N=C5)C=NC4=CC=C3)=C1.Cl.Cl |
| Synonyms | BSK805; NVPBSK805; NVP-BSK805; NVP BSK805; BSK-805; BSK 805; NVPBSK805 dihydrochloride; NVP-BSK805 dihydrochloride; NVP BSK805 dihydrochloride; NVP-BSK805 2HCl; |
| Protocol | 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. |
|---|---|---|
| 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. NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.7747 mL | 8.8736 mL | 17.7472 mL | 35.4943 mL |
| 5mM | 0.3549 mL | 1.7747 mL | 3.5494 mL | 7.0989 mL |
| 10mM | 0.1775 mL | 0.8874 mL | 1.7747 mL | 3.5494 mL |
| 20mM | 0.0887 mL | 0.4437 mL | 0.8874 mL | 1.7747 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.