>>Signaling Pathways>> JAK/STAT Signaling>> JAK>>JAK1-IN-3

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

Catalog No.GC33036

JAK1-IN-3(AZD4205)은 선택적 JAK1 억제제로 IC50이 73nM이고 JAK2를 약하게 억제하며(IC50>14.7 μM) JAK3에 대한 억제가 거의 없습니다(IC50>30 77787788;

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JAK1-IN-3 Chemical Structure

Cas No.: 2091134-68-6

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$194.00
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5mg
US$180.00
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10mg
US$306.00
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50mg
US$810.00
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100mg
US$1,305.00
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고객 리뷰

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

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