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。

JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC 50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC 50 of 896 nM) and JAK2 (IC 50 of 1050 nM).

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JAK3 4.8 nM (IC50) JAK1 896 nM (IC50

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 (IC50

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.

In Vitro: DMSO : 100 mg/mL (196.84 mM; Need ultrasonic)配制储备液