产品
编 号：F752301
分子式：C23H23N5O2
分子量：401.46
分子式：C23H23N5O2
分子量：401.46
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CAS No: 2412734-00-8
产品详情
生物活性：
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.
体内研究：
JAK3-IN-11 (Compound 12) (Oxazolone (OXZ)-induced DTH Balb/c mice; 0-30 mg/kg; PO, prior to and during the challenge phase, 6 days) inhibits oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner.Animal Model:Oxazolone (OXZ)-induced DTH Balb/c mice model.
Dosage:30, 10, and 3 mg/kg.
Administration:PO, prior to and during the challenge phase, 6 days.
Result:Inhibited oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner.
Animal Model:Male ICR mice.
Dosage:30 mg/kg for oral gavage, 10 mg/kg for intravenous administration.
Administration:Pharmacokinetic Analysis
Result:Preliminary pharmacokinetic data of JAK3-IN-11 (Compound 12) in male ICR MiceMale ICR mice, 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration. Compound 12iv (10 mg/kg) po (30 mg/kg)
AUC(0-t) (mg/L*h)a1244.41 ± 77.83889.42 ± 48.32
AUC(0-∞) (mg/L*h)1274.41 ± 57.18 897.12 ± 56.72
MRT (0-∞) (h)b0.73 ± 0.081.42 ± 0.38
Vz (L/kg)c8.36 ± 1.83 220.42 ± 24.71
CLz (L/h/kg)d8.15 ± 1.21 97.14 ± 20.87
t1/2 (h)e0.47 ± 0.061.52 ± 0.34
Cmax (mg/L)f8763.23 ± 324.652008.21 ± 189.44
Bioavailability(%)g23.82%
a Area under the concentration time curve. 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%.
体外研究：
JAK3-IN-11 (Compound 12) (10 μM, 72 h) has no obvious cytotoxicity at a concentration of 10 μM.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).JAK3-IN-11 (Compound 12) (0-10 μM, 1h) abrogates IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner.JAK3-IN-11 (Compound 12) covalently binds to JAK3 and irreversibly inhibits JAK3.
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.
体内研究：
JAK3-IN-11 (Compound 12) (Oxazolone (OXZ)-induced DTH Balb/c mice; 0-30 mg/kg; PO, prior to and during the challenge phase, 6 days) inhibits oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner.Animal Model:Oxazolone (OXZ)-induced DTH Balb/c mice model.
Dosage:30, 10, and 3 mg/kg.
Administration:PO, prior to and during the challenge phase, 6 days.
Result:Inhibited oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner.
Animal Model:Male ICR mice.
Dosage:30 mg/kg for oral gavage, 10 mg/kg for intravenous administration.
Administration:Pharmacokinetic Analysis
Result:Preliminary pharmacokinetic data of JAK3-IN-11 (Compound 12) in male ICR MiceMale ICR mice, 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration. Compound 12iv (10 mg/kg) po (30 mg/kg)
AUC(0-t) (mg/L*h)a1244.41 ± 77.83889.42 ± 48.32
AUC(0-∞) (mg/L*h)1274.41 ± 57.18 897.12 ± 56.72
MRT (0-∞) (h)b0.73 ± 0.081.42 ± 0.38
Vz (L/kg)c8.36 ± 1.83 220.42 ± 24.71
CLz (L/h/kg)d8.15 ± 1.21 97.14 ± 20.87
t1/2 (h)e0.47 ± 0.061.52 ± 0.34
Cmax (mg/L)f8763.23 ± 324.652008.21 ± 189.44
Bioavailability(%)g23.82%
a Area under the concentration time curve. 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%.
体外研究：
JAK3-IN-11 (Compound 12) (10 μM, 72 h) has no obvious cytotoxicity at a concentration of 10 μM.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).JAK3-IN-11 (Compound 12) (0-10 μM, 1h) abrogates IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner.JAK3-IN-11 (Compound 12) covalently binds to JAK3 and irreversibly inhibits JAK3.
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