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CAS No. : 1805787-93-2
MCE 国际站:JAK3-IN-1
产品活性:JAK3-IN-1 是一种有效,选择性和口服活性的 JAK3 抑制剂,IC50 为 4.8 nM。与 JAK1 (IC50 为 896 nM) 和 JAK 2 (IC50 为 1050 nM) 相比,JAK3-IN-1 对 JAK3 的选择性高 180 倍以上。
研究领域:Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点:JAK
In Vitro: JAK3-IN-1(Compound 9; 0-5 µM; 3 hours; BMDMs cells) treatment completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM.
.JAK3-IN-1(Compound 9) most potently inhibits JAK3 and identified fms-related tyrosine kinase 3 (FLT3) and several tyrosine protein kinase (TEC)-family kinases as being potential off-targets. Enzymatic assays using the Z’-lyte or LanthaScreen formats confirmed enzymatic inhibition of FLT3 (IC50 = 13 nM), TTK protein kinase (TTK, IC50 = 49 nM), BLK proto-oncogene (BLK, IC50 = 157 nM) and tyrosine protein kinase TXK (TXK, IC50 = 36 nM). JAK3-IN-1 shows very low inhibition scores for other JAKs and wild-type (WT) EGFR, which is consistent with the over 180-fold higher IC50s against EGFRWT and TYK2 (IC50s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC50s for BTK or ITK (IC50s = 794 and 1070 nM respectively).
JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC50 = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM.
In Vivo: JAK3-IN-1(Compound 9) shows reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10 mg/Kg oral dose and good oral bioavailability of 66%. After oral administration with JAK3-IN-1(Compound 9) (75 mpk, QD) for 8 days, the numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, however, the number of NK cells is reduced.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | 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 | Highly Selective Inhibitors Library | JAK-IN-20 | JAK1-IN-9 | AT9283 | RO495 | TK4b | JAK-IN-17 | (E/Z)-Zotiraciclib | JAK-IN-10 | (3R,4S)-Tofacitinib | JAK3/BTK-IN-6 | Tyk2-IN-5 | Brevilin A | Broussonin E | Itacnosertib | RO8191 | Axltide | Fosifidancitinib | JAK3-IN-6 | Upadacitinib | JAK-IN-24 | AZD-1480 | Baricitinib-d3 | Tofacitinib-13C3 | AZ-3 | Delphinidin chloride | TK4g | Tofacitinib Prodrug-1
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货号: HY-19544
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