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JAK2-IN-7

Catalog No. T35900 CAS 2593402-36-7

Synonyms: JAK2-IN-7

JAK2-IN-7, a selective inhibitor targeting Janus Kinase 2 (JAK2), exhibits inhibitory concentrations (IC50) of 3 nM for JAK2, 11.7 nM for SET-2 cells, and 41 nM for Ba/F3 V617F cells, indicative of its potency and selectivity. This compound demonstrates more than 14-fold selectivity against JAK1, JAK3, and FLT3, underlining its specificity. JAK2-IN-7 effectively induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in tumor cells, manifesting significant antitumor activities [1].

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JAK2-IN-7, CAS 2593402-36-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 148.00
5 mg	In stock	$ 372.00
10 mg	In stock	$ 663.00
25 mg	In stock	$ 1,370.00
50 mg	In stock	$ 1,830.00
100 mg	In stock	$ 2,480.00
1 mL * 10 mM (in DMSO)	In stock	$ 376.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	JAK2-IN-7, a selective inhibitor targeting Janus Kinase 2 (JAK2), exhibits inhibitory concentrations (IC50) of 3 nM for JAK2, 11.7 nM for SET-2 cells, and 41 nM for Ba/F3 V617F cells, indicative of its potency and selectivity. This compound demonstrates more than 14-fold selectivity against JAK1, JAK3, and FLT3, underlining its specificity. JAK2-IN-7 effectively induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in tumor cells, manifesting significant antitumor activities [1].
In vitro	JAK2-IN-7 (compound 13ac), in concentrations ranging from 0-1000 nM for 2 hours, dose-dependently inhibits the phosphorylation of JAK2 and STAT5 in both SET-2 and Ba/F3-JAK2 V617F cells. Additionally, at 10-160 nM over 24 hours, it promotes cell cycle arrest at the G0/G1 phase, and at 0.05-1.6 μM for 2 hours, it induces apoptosis in SET-2 cells. Both the cell cycle arrest and apoptosis induction are concentration-dependent, confirming the compound's efficacy in modulating key cellular processes related to proliferation and survival.
In vivo	JAK2-IN-7, administered orally at doses ranging from 15 to 60 mg/kg daily for 16 days, demonstrated strong antitumor activity, inhibiting tumor growth by 82.3% in the SET-2 xenograft model [1]. At doses between 30 and 60 mg/kg, it significantly reduced disease symptoms in a Ba/F3-JAK2V617F allograft model by normalizing spleen weight by 77.1%, outperforming Ruxolitinib [1]. These findings, derived from administering JAK2-IN-7 to a NOD/SCID mouse model inoculated with SET-2 cells, highlight its potential without noticeable weight changes in the animals.

Synonyms	JAK2-IN-7
Molecular Weight	459.59
Formula	C26H33N7O
CAS No.	2593402-36-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (543.96 mM), Sonication is recommended.

References and Literature

1. Yang T, et al. N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms [published online ahead of print, 2020 Nov 30]. J Med Chem. 2020;10.1021/acs.jmedchem.0c01488.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Anti-Liver Cancer Compound Library Bioactive Compounds Library Max Anti-Lung Cancer Compound Library Anti-Cancer Compound Library Anti-Prostate Cancer Compound Library

Related Products

Related compounds with same targets

JAK-IN-33 Lorpucitinib 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide CEP-33779 Solcitinib ON123300 JAK-IN-34 WHI-P97 HCl 211555-05-4(free base)

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Keywords

JAK2-IN-7 2593402-36-7 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK JAK2IN7 JAK-2-IN-7 JAK2 IN 7 inhibitor inhibit

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