1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. JAK
  3. JAK1-IN-13

JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC50 of 0.044 nM. JAK1-IN-13 significantly decreases STAT3 phosphorylation.

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JAK1-IN-13

JAK1-IN-13 Chemische Struktur

CAS. Nr. : 2778330-90-6

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Beschreibung

JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC50 of 0.044 nM. JAK1-IN-13 significantly decreases STAT3 phosphorylation[1].

Cellular Effect
Cell Line Type Value Description References
BaF3 GI50
0.001 μM
Compound: 36b
Growth inhibition of mouse BaF3 cells harboring JAK1 measured after 72 hrs by CCK-8 assay
Growth inhibition of mouse BaF3 cells harboring JAK1 measured after 72 hrs by CCK-8 assay
[PMID: 38031930]
BaF3 GI50
0.174 μM
Compound: 36b
Growth inhibition of mouse BaF3 cells harboring TYK2 measured after 72 hrs by CCK-8 assay
Growth inhibition of mouse BaF3 cells harboring TYK2 measured after 72 hrs by CCK-8 assay
[PMID: 38031930]
BaF3 GI50
0.577 μM
Compound: 36b
Growth inhibition of mouse BaF3 cells harboring JAK2 measured after 72 hrs by CCK-8 assay
Growth inhibition of mouse BaF3 cells harboring JAK2 measured after 72 hrs by CCK-8 assay
[PMID: 38031930]
BaF3 GI50
1.41 μM
Compound: 36b
Growth inhibition of mouse BaF3 cells harboring JAK3 measured after 72 hrs by CCK-8 assay
Growth inhibition of mouse BaF3 cells harboring JAK3 measured after 72 hrs by CCK-8 assay
[PMID: 38031930]
L132 IC50
60 μM
Compound: 36b
Cytotoxicity against human L132 cells assessed as inhibition of cell growth measured after 24 hrs by MTT colorimetric assay
Cytotoxicity against human L132 cells assessed as inhibition of cell growth measured after 24 hrs by MTT colorimetric assay
[PMID: 38031930]
Molekulargewicht

445.48

Formel

C23H26F3N5O

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(N[C@@H]2C[C@@H](N(CC2)CC3=CC=C(C=C3)C(F)(F)F)C)C4=C(NC=C4)N=C1)NC

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (224.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2448 mL 11.2238 mL 22.4477 mL
5 mM 0.4490 mL 2.2448 mL 4.4895 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2448 mL 11.2238 mL 22.4477 mL 56.1192 mL
5 mM 0.4490 mL 2.2448 mL 4.4895 mL 11.2238 mL
10 mM 0.2245 mL 1.1224 mL 2.2448 mL 5.6119 mL
15 mM 0.1497 mL 0.7483 mL 1.4965 mL 3.7413 mL
20 mM 0.1122 mL 0.5612 mL 1.1224 mL 2.8060 mL
25 mM 0.0898 mL 0.4490 mL 0.8979 mL 2.2448 mL
30 mM 0.0748 mL 0.3741 mL 0.7483 mL 1.8706 mL
40 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4030 mL
50 mM 0.0449 mL 0.2245 mL 0.4490 mL 1.1224 mL
60 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
80 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7015 mL
100 mM 0.0224 mL 0.1122 mL 0.2245 mL 0.5612 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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