Cat. No.: HY-19544

JAK3-IN-1

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Based on 1 Customer Validation

JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC₅₀ of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC₅₀ of 896 nM) and JAK2 (IC₅₀ of 1050 nM).

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

Purity: 99.31%
CAS No.: 1805787-93-2
Formula: C₂₆H₃₀ClN₇O₂
Molecular Weight:508.02

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

JAK3-IN-1 Chemical Structure

CAS No.: 1805787-93-2

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK3

4.8 nM (IC₅₀)

JAK1

896 nM (IC₅₀)

JAK2

1050 nM (IC₅₀)

TTK

49 nM (IC₅₀)

BTK

794 nM (IC₅₀)

ITK

1070 nM (IC₅₀)

All JAK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	2266 nM Compound: 9	Antiproliferative activity against mouse BA/F3 cells expressing TYK2 E957D mutant after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TYK2 E957D mutant after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	IC₅₀	3047 nM Compound: 9	Antiproliferative activity against mouse BA/F3 cells expressing TEL-ABL after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-ABL after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	IC₅₀	3124 nM Compound: 9	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK1 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK1 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	IC₅₀	3194 nM Compound: 9	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK2 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK2 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	IC₅₀	69 nM Compound: 9	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	[PMID: 26258521]

In Vitro

JAK3-IN-1(Compound 9; 0-5 µM; 3 hours; BMDMs cells) treatment completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM^[1].
. JAK3-IN-1(Compound 9) most potently inhibits JAK3 and identified fms-related tyrosine kinase 3 (FLT3) and several tyrosine protein kinase (TEC)-family kinases as being potential off-targets. Enzymatic assays using the Z’-lyte or LanthaScreen formats confirmed enzymatic inhibition of FLT3 (IC₅₀ = 13 nM), TTK protein kinase (TTK, IC₅₀ = 49 nM), BLK proto-oncogene (BLK, IC₅₀ = 157 nM) and tyrosine protein kinase TXK (TXK, IC₅₀ = 36 nM). JAK3-IN-1 shows very low inhibition scores for other JAKs and wild-type (WT) EGFR, which is consistent with the over 180-fold higher IC₅₀s against EGFRWT and TYK2 (IC₅₀s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC₅₀s for BTK or ITK (IC₅₀s = 794 and 1070 nM respectively)^[1].
JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC₅₀ = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

BMDMs cells
Concentration:

0 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM
Incubation Time:

3 hours
Result:

Completely inhibited IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibited IFNβ-induced p-STAT1 at a concentration of 5.0 μM.

In Vivo

JAK3-IN-1(Compound 9) shows reasonable pharmacokinetic properties, with moderate T_1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10 mg/Kg oral dose and good oral bioavailability of 66%. After oral administration with JAK3-IN-1(Compound 9) (75 mpk, QD) for 8 days, the numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, however, the number of NK cells is reduced^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1805787-93-2
Appearance Solid
Molecular Weight 508.02
Formula C₂₆H₃₀ClN₇O₂
Color White to off-white
SMILES

O=C(C=C)NC1=CC(CNC2=NC(NC3=C(OC)C=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (196.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9684 mL

9.8421 mL

19.6843 mL

5 mM

0.3937 mL

1.9684 mL

3.9369 mL

10 mM

0.1968 mL

0.9842 mL

1.9684 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: 2.5 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (4.92 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9684 mL	9.8421 mL	19.6843 mL	49.2107 mL
	5 mM	0.3937 mL	1.9684 mL	3.9369 mL	9.8421 mL
	10 mM	0.1968 mL	0.9842 mL	1.9684 mL	4.9211 mL
	15 mM	0.1312 mL	0.6561 mL	1.3123 mL	3.2807 mL
	20 mM	0.0984 mL	0.4921 mL	0.9842 mL	2.4605 mL
	25 mM	0.0787 mL	0.3937 mL	0.7874 mL	1.9684 mL
	30 mM	0.0656 mL	0.3281 mL	0.6561 mL	1.6404 mL
	40 mM	0.0492 mL	0.2461 mL	0.4921 mL	1.2303 mL
	50 mM	0.0394 mL	0.1968 mL	0.3937 mL	0.9842 mL
	60 mM	0.0328 mL	0.1640 mL	0.3281 mL	0.8202 mL
	80 mM	0.0246 mL	0.1230 mL	0.2461 mL	0.6151 mL
	100 mM	0.0197 mL	0.0984 mL	0.1968 mL	0.4921 mL

Keywords

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JAK3-IN-1

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

All JAK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

JAK3-IN-1 Related Classifications

Cat. No.: HY-19544