JAK3-IN-11
JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.
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- CAS No.: 2412734-00-8
- 화학식: C23H23N5O2
- 분자량:401.46
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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JAK3 1.7 nM (IC50) |
JAK2 1 μM (IC50) |
JAK1 1.32 μM (IC50) |
JAK3-IN-11 (Compound 12) (10 μM, 72 h) has no obvious cytotoxicity at a concentration of 10 μM[1].
JAK3-IN-11 (Compound 12) (72 h) displays strong inhibition for T cell proliferation with IC50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation)[1].
JAK3-IN-11 (Compound 12) (0-10 μM, 1h) abrogates IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner[1].
JAK3-IN-11 (Compound 12) covalently binds to JAK3 and irreversibly inhibits JAK3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse T cells in complete RPMI1640 medium then exposed to anti-CD3/anti-CD28 or IL-2.
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Concentration:
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Incubation Time:72 h.
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Result:Displayed strong inhibition for T cell proliferation with an IC50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation), showed obvious significant immunosuppressive activity under selective inhibition of JAK3.
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Cell Line:Purified T cells were pre-activated coated with anti-CD3 and anti-CD28 for 72 h, then cultured with IL-2 (50 U/mL) for 36 h, then, cultured without IL-2 for 36 h
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Concentration:0.01, 0.1, 1, 10 μM.
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Incubation Time:1 h.
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Result:Abrogated IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Oxazolone (OXZ)-induced DTH Balb/c mice model[1].
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Dosage:30, 10, and 3 mg/kg.
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Administration:PO, prior to and during the challenge phase, 6 days.
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Result:Inhibited oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner.
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Animal Model:Male ICR mice[1].
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Dosage:30 mg/kg for oral gavage, 10 mg/kg for intravenous administration.
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Administration:Pharmacokinetic Analysis
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Result:Preliminary pharmacokinetic data of JAK3-IN-11 (Compound 12) in male ICR Mice[1]
Male ICR mice, 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration[1].
a Area under the concentration time curve.Compound 12 iv (10 mg/kg) po (30 mg/kg) AUC(0-t) (mg/L*h)a 1244.41 ± 77.83 889.42 ± 48.32 AUC(0-∞) (mg/L*h) 1274.41 ± 57.18 897.12 ± 56.72 MRT (0-∞) (h)b 0.73 ± 0.08 1.42 ± 0.38 Vz (L/kg)c 8.36 ± 1.83 220.42 ± 24.71 CLz (L/h/kg)d 8.15 ± 1.21 97.14 ± 20.87 t1/2 (h)e 0.47 ± 0.06 1.52 ± 0.34 Cmax (mg/L)f 8763.23 ± 324.65 2008.21 ± 189.44 Bioavailability(%)g 23.82%
b Mean residence time.
c Volume in steady state.
d Plasma clearance.
e Terminal half-life.
f Peak plasma concentrations.
g Bioavailability = AUC0-t(po)/AUC0-t × 100%.
Chemical Information
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CAS No. 2412734-00-8
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분자량 401.46
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화학식 C23H23N5O2
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SMILES
C=CC(NC1=CC=C(C=C1)C2=NC(NC3=CC=C(C=C3)N4CCOCC4)=NC=C2)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK3-IN-11 Related Classifications
HY-146727 Related Classifications
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