1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. JAK1-IN-3

JAK1-IN-3 

Cat. No.: HY-107361 Purity: 99.32%
Handling Instructions

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).

For research use only. We do not sell to patients.

JAK1-IN-3 Chemical Structure

JAK1-IN-3 Chemical Structure

CAS No. : 2091134-68-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 715 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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).

IC50 & Target[1]

JAK1

73 nM (IC50)

In Vitro

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].

In Vivo

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].

Molecular Weight

489.57

Formula

C₂₅H₃₁N₉O₂

CAS No.

2091134-68-6

SMILES

C[[email protected]@H](N1CCN(C)CC1)C(NC2=C3C(C(C4=NC(NC5=CN(C)N=C5OC)=NC=C4)=CN3)=CC=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (510.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0426 mL 10.2130 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.32%

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Keywords:

JAK1-IN-3JAKJanus kinaseInhibitorinhibitorinhibit

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Product name:
JAK1-IN-3
Cat. No.:
HY-107361
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