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JAK3-IN-1

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 T_1/2 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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