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JAK1-IN-3 (Synonyms: Golidocitinib; AZD4205)

カタログ番号GC33036

JAK1-IN-3 (AZD4205) は選択的 JAK1 阻害剤であり、IC50 は 73 nM で、JAK2 を弱く阻害し (IC50>14.7 μM)、JAK3 をほとんど阻害しません (IC50>30 μM)。

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JAK1-IN-3 化学構造

Cas No.: 2091134-68-6

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$194.00
在庫あり
5mg
$180.00
在庫あり
10mg
$306.00
在庫あり
50mg
$810.00
在庫あり
100mg
$1,305.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

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
同義語 Golidocitinib; AZD4205
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
溶解度 DMSO: 250 mg/mL (510.65 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.0426 mL 10.213 mL 20.4261 mL
5 mM 0.4085 mL 2.0426 mL 4.0852 mL
10 mM 0.2043 mL 1.0213 mL 2.0426 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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