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JAK3-IN-13
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
JAK3-IN-13图片
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
JAK3-IN-13 是一种有效、选择性和口服活性的JAK3抑制剂，对 NK1、JNK2、JNK3、Tyk2 的IC50值分别为 4728、2039、8、365 nM。JAK3-IN-13 显示出抗增殖活性。JAK3-IN-13诱导细胞周期停滞在 G0/G1 期。JAK3-IN-13 具有抗肿瘤活性。
生物活性

JAK3-IN-13 is a potent, selective and orally activeJAK3inhibitor withIC50values of 4728, 2039, 8, 365 nM forNK1,JNK2,JNK3,Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity[1].

IC50& Target[1]

JNK1

4728 nM (IC50)

JNK2

2039 nM (IC50)

JNK3

8 nM (IC50)

Tyk2

365 nM (IC50)

体外研究
(In Vitro)

JAK3-IN-13 (compound 12n) (10 μM; 72 h) shows antiproliferative activity in BaF3-JAK3M511I, U937, parental cells[1].
JAK3-IN-13 inhibits the activity of TEL-JNK1, TEL-JNK2, JNK3M511I, JNK3 with IC50values of 177.7, 134.2, 22.9, 1.2 nM, respectively[1].
JAK3-IN-13 inhibits (0-800 nM; 0-24 h) decreases the expression of phosphorylation JAK3, STAT3, and STAT5 in a dose-dependent manner[1].
JAK3-IN-13 inhibits (0-330 nM; 24 h) induces cell cycle arrest at G0/G1 phase and down-regulates the expression of cyclin-dependent kinase 2 (CDK2), CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1 in a concentration-dependent manner[1].

Cell Proliferation Assay[1]

Cell Line:BaF3-JAK3M511I, U937, parental, COLO-205, H1299, HCT-116, MDA-MB-231, AGS, HL 7702 cells
Concentration:10 μM
Incubation Time:72 h
Result:Showed antiproliferative activity with IC50s of 22.9, 20.2, 165.1 nM for BaF3-JAK3M511I, U937, parental cells, and >10, >10, >10, >10, >10, 3.27 μM for COLO-205, H1299, HCT-116, MDA-MB-231, AGS, HL 7702 cells, respectively.

Western Blot Analysis[1]

Cell Line:U937 cells
Concentration:0-800 nM
Incubation Time:0-24 h
Result:Dose-dependently suppressed the phosphorylation of JAK3, STAT3, and STAT5 and achieved near-complete inhibition at 200 nM.

Cell Cycle Analysis[1]

Cell Line:U937 cells
Concentration:0-330 nM
Incubation Time:24 h
Result:Induced cell cycle arrest at G0/G1 phase and down-regulated the expression of cyclin-dependent kinase 2 (CDK2), CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1 in a concentration-dependent manner.
体内研究
(In Vivo)

JAK3-IN-13 (5 mg/kg for i.v.; 15 mg/kg for p.o.) shows good PK properties and oral bioavailability of 20.66%[1].
JAK3-IN-13 (12.5, 25, 50 mg/kg; p.o.; twice daily for 10 days) shows antitumor activity and inhibits the expression of phosphorylation JAK3, STAT3, STAT5, CDK2, CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1[1].Pharmacokinetic Parameters of JAK3-IN-13 in Male Sprague-Dawley rats[1].

12ni.v.(5 mg/kg)p.o.(15 mg/kg)
anminal no.33
T1/2(h)0.910.98
Cmax(ng/mL)911.33238.28
AUC(0-∞)(h·ng/mL)536.99333.50
CL (mL/min/kg)155.22
F %20.66
Male Sprague-Dawley rats, 5 mg/kg iv (5% DMSO + 10% solutol + 85% saline); 15 mg/kg po (0.5% HPMC in water)[1]

Animal Model:Male Sprague-Dawley rats[1]
Dosage:5 mg/kg for i.v.; 15 mg/kg for p.o.
Administration:I.v. or p.o.
Result:Showed good PK properties and oral bioavailability of 20.66%.
Animal Model:Male CB17-SCID mice (U937 mouse xenograft model)[1]
Dosage:12.5, 25, 50 mg/kg
Administration:P.o.; twice daily for 10 days (10 mg/kg; i.p.; once daily)
Result:Dose-dependently inhibited the growth of the U937 tumor and significantly inhibited the expression of phosphorylation JAK3, STAT3, and STAT5 as well as the cell cycle-related proteins.
分子量

533.02

Formula

C25H33ClN6O5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.