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Chemical Structure| 1092499-93-8 Chemical Structure| 1092499-93-8

Structure of NVP-BSK805
CAS No.: 1092499-93-8

Chemical Structure| 1092499-93-8

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NVP-BSK805 is a selective JAK2 and JAK2(V617F) mutant inhibitor with IC50 value of 0.48 nM, with >20-fold selectivity over TYK2, JAK3 and JAK1 (IC50 values of 10.8, 18.7 and 31.6 nM, respectively).

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Product Details of NVP-BSK805

CAS No. :1092499-93-8
Formula : C27H28F2N6O
M.W : 490.55
SMILES Code : FC1=C(C(F)=CC(C2=C3N=C(C4=CN(C5CCNCC5)N=C4)C=NC3=CC=C2)=C1)CN6CCOCC6
MDL No. :MFCD22419018
InChI Key :IBPVXAOOVUAOKJ-UHFFFAOYSA-N
Pubchem ID :46398810

Safety of NVP-BSK805

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of NVP-BSK805

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Description
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, 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[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
MB-02 cells 500 nM 16 hours To study the effect of NVP-BSK805 on apoptosis in JAK2V617F mutant cells, results showed that NVP-BSK805 induced Bim activation and decreased Mcl-1 levels. BMC Cancer. 2011 Jan 19;11:24
KBV20C cells 2 µM 24 hours To evaluate the cytotoxic effects of NVP-BSK805 in combination with vincristine (VIC) on KBV20C cells. Results showed that NVP-BSK805 co-treatment with VIC significantly increased apoptosis in KBV20C cells. Int J Mol Sci. 2022 Apr 21;23(9):4597.
SET-2 cells 500 nM 24 hours To study the effect of NVP-BSK805 on apoptosis in JAK2V617F mutant cells, results showed that NVP-BSK805 induced Bim activation and decreased Mcl-1 levels. BMC Cancer. 2011 Jan 19;11:24
KYSE-180 cells 5 µM and 10 µM 4 hours NVP-BSK805 significantly enhanced the radiosensitivity of KYSE-180 cells. Drug Des Devel Ther. 2020 Feb 24;14:745-755
KYSE-30 cells 5 µM and 10 µM 4 hours NVP-BSK805 significantly enhanced the radiosensitivity of KYSE-30 cells. Drug Des Devel Ther. 2020 Feb 24;14:745-755
KYSE-150R cells 10 µM 4 hours NVP-BSK805 significantly increased γ-H2AX expression and inhibited DNA damage repair. Drug Des Devel Ther. 2020 Feb 24;14:745-755
RT112 0.0125 to 1 µM 72 hours To evaluate the effect of BSK-805 on bladder cancer cell growth, results showed inhibition of cell growth only in T24, J82, and RT112 cells Int J Mol Sci. 2020 Feb 7;21(3):1106
J82 0.0125 to 1 µM 72 hours To evaluate the effect of BSK-805 on bladder cancer cell growth, results showed inhibition of cell growth only in T24, J82, and RT112 cells Int J Mol Sci. 2020 Feb 7;21(3):1106
T24 0.0125 to 1 µM 72 hours To evaluate the effect of BSK-805 on bladder cancer cell growth, results showed inhibition of cell growth only in T24, J82, and RT112 cells Int J Mol Sci. 2020 Feb 7;21(3):1106

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Healthy mice Intraperitoneal or intracerebroventricular 0.03 mg (ip) or 3.12 mg/mL (icv) Daily ip injection for 10 days, then twice-daily for a total of 21 days; or weekly icv injection for 3 weeks To evaluate the effects of NVP-BSK805 on food intake, body weight, and body composition. Results showed that chronic peripheral administration increased fat mass and feed efficiency, while icv administration had more pronounced effects. Acute icv administration blocked leptin-induced anorexia and weight loss by inhibiting hypothalamic STAT3 phosphorylation. Front Pharmacol. 2018 May 15;9:527
BALB/c nude mice KYSE-150 xenograft model Gavage 30 mg/kg 11 consecutive days NVP-BSK805 combined with radiotherapy significantly delayed tumor growth time (59 days vs 37 days). Drug Des Devel Ther. 2020 Feb 24;14:745-755

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.19mL

2.04mL

1.02mL

20.39mL

4.08mL

2.04mL

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