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Art. -Nr.: HY-143444

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JAK-IN-20

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Based on 1 Customer Validation

JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC₅₀s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.

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Reinheit: 99.63%
CAS. Nr.: 1654776-91-6
Formel: C₂₈H₃₀FN₇O₂
Molecular Weight:515.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

JAK-IN-20 Chemical Structure

CAS. Nr.: 1654776-91-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

JAK1

7 nM (IC₅₀)

JAK2

5 nM (IC₅₀)

JAK3

14 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

In Vivo

JAK-IN-20 (compound 32) (3 mg/kg for p.o.; 1 mg/kg for i.v.) shows excellent pharmacokinetics in rats^[1].
JAK-IN-20 (10 mg/kg; p.o.; once a day for 3 days) shows anti-inflammatory effect^[1].
Pharmacokinetic Parameters of JAK-IN-20 in female Sprague Dawley rats^[1].

parameter	32
PO Dose (mg/kg)	3
T_max (h)	0.63(0.25-6)
C_max (μg/mL)	7.82±3.68
AUC_0-t (μg.h/mL)	80.18±35.44
T^1/2,po (h)	4.77±1.84
MRT (h)	7.54±2.52
IV Dose (mg/kg)	1
C₀ (μg/mL)	4.70±2.50
AUC_0-t (μg.h/mL)	18.89±1.76
V_ss (L/kg)	0.32±0.14
CL (mL/min/kg)	0.85±0.13
T^1/2,iv (h)	5.16±3.83
MRT (h)	6.69±4.03
%F	100

Wistar rats; 3 mg/kg; p.o. (1% Tween 80 + 99% (0.5%) methyl cellulose in water); 1 mg/kg; i.v. (5% NMP + 5% solutol + 90% normal saline)^[1]

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

Animal Model:

7-10 weeks, 250-300g, male wistar rats^[1]
Dosage:
Administration:

3 mg/kg for p.o.; 1 mg/kg for i.v.
Result:

Showed fast oral absorption, higher plasma exposure, extended oral half-life and excellent oral bioavailability of 100%.

Animal Model:

Female Sprague Dawley rats ( PGPS rat model)^[1]
Dosage:

10 mg/kg
Administration:

P.o.; once a day; 3 days
Result:

Showed anti-inflammatory effect.

Chemical Information

CAS. Nr. 1654776-91-6
Appearance Solid
Molecular Weight 515.58
Formel C₂₈H₃₀FN₇O₂
Color Light yellow to yellow
SMILES

O=C(NCC#N)C1=CC=C(C2=NC(NC3=CC=C(N4CCC(N5CCOCC5)CC4)C=C3)=NC=C2F)C=C1
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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)
- Korean - KR (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)

Verweise

[1]. Desai J, et al. Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitor. Bioorg Med Chem Lett. 2022; 66:128728. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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JAK-IN-20

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

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

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

JAK-IN-20 Related Classifications

HY-143444 Related Classifications