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JAK1-IN-3

Catalog No.GC33036

JAK1-IN-3 Chemical Structure

Size Price Stock Qty
10mM * 1mL in DMSO
$194.00
In stock
5mg
$180.00
In stock
10mg
$306.00
In stock
50mg
$810.00
In stock
100mg
$1,305.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Background

JAK1-IN-3 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively).

JAK1-IN-3 (Example 32) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively). JAK1-IN-3 significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC50 of 161 nM[1].

JAK1-IN-3 (12.5 mg/kg BID (twice daily), 25 m/kg BID or 50 mg/kg BID, p.o.) alone has increasing antitumor effects, and ehances the antitumor activity of osimertinib, compared to treatment with osimertinib alone in mice bearing NCI-H1975 cells[1].

[1]. Annika Birgitta Margareta ?STRAND, et al. Compounds and methods for inhibiting jak.

Chemical Properties

Cas No. 2091134-68-6 SDF
Synonyms Golidocitinib; AZD4205
Chemical Name N/A
Canonical SMILES C[C@@H](N1CCN(C)CC1)C(NC2=C3C(C(C4=NC(NC5=CN(C)N=C5OC)=NC=C4)=CN3)=CC=C2)=O
Formula C25H31N9O2 M.Wt 489.57
Solubility DMSO: 250 mg/mL (510.65 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Reviews

Review for JAK1-IN-3

Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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