1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. JAK
  3. JAK-IN-21

JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively.

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

JAK-IN-21 Chemical Structure

JAK-IN-21 Chemical Structure

CAS No. : 2445499-20-5

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5 mg USD 650 In-stock
10 mg USD 995 In-stock
25 mg USD 1990 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively[1].

IC50 & Target[1]

JAK1

1.73 nM (IC50)

JAK2

2.04 nM (IC50)

Tyk2

62.9 nM (IC50)

JAK2-V617F

109 nM (IC50)

In Vitro

JAK-IN-21 (Example 4) doses not inhibit CYPs and shows good liver microsome stability[1].

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

In Vivo

JAK-IN-21 (Example 4) shows low bioavailability (F=1.9%)[1].

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

Animal Model: SD rats[1]
Dosage: 10 mg/kg
Administration: Oral gavage (Pharmacokinetic Study)
Result: Rat Colon Pharmacokinetic Study[1]
Compound Plasma Cmax
(ng/mL)
Plasma AUC
(h*ng/mL)
t1/2 (h) Colon AUC
(h*ng/g)
Colon + Feces AUC
(h*ng/g)
JAK-IN-21 68.8 96 1.6 6,623 545,501
Animal Model: SD rats[1]
Dosage: 1 mg/kg or 2 mg/kg
Administration: Intravenous injection (1 mg/kg) or oral gavage (2 mg/kg) (Pharmacokinetic Study)
Result: Pharmacokinetic Parameters in Sprague-Dawley Rats by Intravenous Administration and Oral Administration[1]
Compound Dose
(mg/kg)
AUC
(h*ng/mL)
T1/2 (h) Cl
(mL/min/kg)
Vd
(L/kg)
Cmax
(ng/mL)
F (%)
JAK-IN-21 (iv) 1 854.8 0.22 19.4 0.37
JAK-IN-21 (ig) 2 29.8 0.38 40.4 1.9
Molecular Weight

372.38

Formula

C19H16N8O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CCNC(C1=CC=C(C2=NC(NC3=CN(CC#N)N=C3)=NC=C2C)C=C1)=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 : 125 mg/mL (335.68 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 2.6854 mL 13.4271 mL 26.8543 mL
5 mM 0.5371 mL 2.6854 mL 5.3709 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.

  • Molarity Calculator

  • Dilution Calculator

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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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 2.6854 mL 13.4271 mL 26.8543 mL 67.1357 mL
5 mM 0.5371 mL 2.6854 mL 5.3709 mL 13.4271 mL
10 mM 0.2685 mL 1.3427 mL 2.6854 mL 6.7136 mL
15 mM 0.1790 mL 0.8951 mL 1.7903 mL 4.4757 mL
20 mM 0.1343 mL 0.6714 mL 1.3427 mL 3.3568 mL
25 mM 0.1074 mL 0.5371 mL 1.0742 mL 2.6854 mL
30 mM 0.0895 mL 0.4476 mL 0.8951 mL 2.2379 mL
40 mM 0.0671 mL 0.3357 mL 0.6714 mL 1.6784 mL
50 mM 0.0537 mL 0.2685 mL 0.5371 mL 1.3427 mL
60 mM 0.0448 mL 0.2238 mL 0.4476 mL 1.1189 mL
80 mM 0.0336 mL 0.1678 mL 0.3357 mL 0.8392 mL
100 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6714 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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Product Name:
JAK-IN-21
Cat. No.:
HY-148060
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