ChemicalBook > CAS DataBase List > NVP-BSK805
NVP-BSK805
NVP-BSK805
- CAS No.1092499-93-8
- Chemical Name:NVP-BSK805
- CBNumber:CB62561486
- Molecular Formula:C27H28F2N6O
- Formula Weight:490.55
- MOL File:1092499-93-8.mol
NVP-BSK805 Property
- Melting point 137℃
- Boiling point 639.8±55.0 °C(Predicted)
- Density 1.4
- storage temp. Store at -20°C
- solubility ≥20.95 mg/mL in DMSO; ≥3.45 mg/mL in H2O with gentle warming and ultrasonic; ≥4.75 mg/mL in EtOH with gentle warming and ultrasonic
- form solid
- pka 9.78±0.10(Predicted)
- color Off-white to yellow
- Symbol(GHS)
- Signal word
- Hazard statements
- Precautionary statements
NVP-BSK805 Chemical Properties,Usage,Production
- Uses 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].
-
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]. - target JAK2
- IC 50 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)
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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. DOI:10.1158/1535-7163.MCT-10-0053
[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. DOI:10.1016/j.bbrc.2017.06.178
NVP-BSK805 Preparation Products And Raw materials
Raw materials
Preparation Products
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1092499-93-8, NVP-BSK805Related Search:
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- Inhibitor
- STAT
- JAK
- Inhibitors
- 抑制剂
- 药靶配体
- 标准品
- 细胞生物学试剂
- 蛋白酪氨酸激酶
- 小分子抑制剂,天然产物
- C27H28F2N6O2HCl
- C27H28F2N6O
- 化合物 NVP-BSK805
- 4-(2,6-二氟-4-(3-(1-(哌啶-4-基)-1H-吡唑-4-基)喹喔啉-5-基)苄基)吗啉
- NVP-BSK805游离态
- JAK2抑制剂(NVP-BSK805 DIHYDROCHLORIDE)
- 8-[3,5-二氟-4-(4-吗啉基甲基)苯基]-2-[1-(4-哌啶基)-1H-吡唑-4-基]喹喔啉
- 1092499-93-8
- 8-{3,5-difluoro-4-[(morpholin-4-yl)methyl]phenyl}-2-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]quinoxaline
- NVP-BSK805(freebase)
- NVP-BSK805 USP/EP/BP
- Quinoxaline, 8-[3,5-difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-
- NVP-GSK 805
- CS-550
- BSK 805; BSK-805; BSK805; NVP-BSK 805
- CS-1571
- NVP-BSK805 - BSK 805
- 4-(2,6-Difluoro-4-(3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxalin-5-yl)benzyl)morpholine
- BSK-805
- BSK805
- BSK 805
- 8-(3,5-difluoro-4-(morpholinomethyl)phenyl)-2-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxaline
- 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline
- NVP-BSK805 dihydrochloride
- NVP-BSK805
- NVP-BSK805 2HCl