2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. JAK-IN-20

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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JAK-IN-20 Chemical Structure

JAK-IN-20 Chemical Structure

CAS No. : 1654776-91-6

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JAK-IN-20 Related Antibodies

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Description

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[1].

IC50 & Target

JAK1

7 nM (IC50)

JAK2

5 nM (IC50)

JAK3

14 nM (IC50)

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
Tmax (h) 0.63(0.25-6)
Cmax (µg/mL) 7.82±3.68
AUC0-t (µg.h/mL) 80.18±35.44
T1/2,po (h) 4.77±1.84
MRT (h) 7.54±2.52
IV Dose (mg/kg) 1
C0 (µg/mL) 4.70±2.50
AUC0-t (µg.h/mL) 18.89±1.76
Vss (L/kg) 0.32±0.14
CL (mL/min/kg) 0.85±0.13
T1/2,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.
Molecular Weight

515.58

Formula

C28H30FN7O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JAK-IN-20 Related Classifications

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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.

Keywords:

JAK-IN-201654776-91-6JAKJanus kinaseanti-inflammatorypanmomelotinibSprague Dawley ratswistar ratsorally activeInhibitorinhibitorinhibit

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