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JAK3-IN-1

COA COA
    级别和纯度:
  • ≥99%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
J647018-5mg
 5mg 期货 Stock Image
J647018-10mg
 10mg 期货 Stock Image
J647018-50mg
 50mg 期货 Stock Image
J647018-100mg
 100mg 期货 Stock Image
大包装询价 收藏夹 比较  SDS下载  DATASHEET  质量标准
查看相关系列
Histone Modification (3105) JAK (149) JAK/STAT Signaling (508) Non-receptor Tyrosine Kinase (1390) Protein Tyrosine Kinase/RTK (1319) Stem Cell/Wnt (1018) 表观遗传学 (1497)
main product photo

基本描述

规格或纯度 ≥99%
英文名称 JAK3-IN-1
生化机理 JAK3-IN-1 是一种强效、选择性和口服活性 JAK3 抑制剂，其 IC 50 为 4.8 nM。与 JAK1（IC 50 为 896 nM）和 JAK2（IC 50 为 1050 nM）相比，JAK3-IN-1 对 JAK3 的选择性高出 180 多倍。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


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)

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. .\nJAK3-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 (IC 50 = 13 nM), TTK protein kinase (TTK, IC 50 = 49 nM), BLK proto-oncogene (BLK, IC 50 = 157 nM) and tyrosine protein kinase TXK (TXK, IC 50 = 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 IC 50 s against EGFRWT and TYK2 (IC 50 s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC 50 s for BTK or ITK (IC 50 s = 794 and 1070 nM respectively). JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC 50 = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: BMDMs cells Concentration: 0 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM Incubation Time: 3 hours Result: Completely inhibited IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibited IFNβ-induced p-STAT1 at a concentration of 5.0 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%.\nAfter 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:JAK3 4.8 nM (IC 50 ) JAK1 896 nM (IC 50 ) JAK2 1050 nM (IC 50 ) TTK 49 nM (IC 50 ) BTK 794 nM (IC 50 ) ITK 1070 nM (IC 50 )
纯度 ≥99%

关联靶点（人）

FLT3 Tclin 受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
JAK3 Tclin 酪氨酸蛋白激酶JAK3(Tyrosine-protein kinase JAK3) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ITK Tclin Tyrosine-protein kinase ITK/TSK (3699 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTK2 Tclin Focal adhesion kinase 1 (4730 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BLK Tchem Tyrosine-protein kinase BLK (2498 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TYK2 Tclin Tyrosine-protein kinase TYK2 (5029 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ERBB4 Tclin Receptor protein-tyrosine kinase erbB-4 (2748 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SGK1 Tchem Serine/threonine-protein kinase Sgk1 (2343 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GAK Tchem Serine/threonine-protein kinase GAK (1150 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TTK Tchem Dual specificity protein kinase TTK (2978 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAMKK2 Tchem CaM-kinase kinase beta (1281 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BTK Tclin Tyrosine-protein kinase BTK (8973 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TXK Tchem Tyrosine-protein kinase TXK (1590 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TNK1 Tchem Non-receptor tyrosine-protein kinase TNK1 (1335 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NUAK1 Tchem NUAK family SNF1-like kinase 1 (1769 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
LTK Tclin Leukocyte tyrosine kinase receptor (1542 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Liver (3974 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Tyk2 Non-receptor tyrosine-protein kinase TYK2 (29 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IIUPAC Name N-[3-[[[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]methyl]phenyl]prop-2-enamide
INCHI 1S/C26H30ClN7O2/c1-4-24(35)30-19-7-5-6-18(14-19)16-28-25-21(27)17-29-26(32-25)31-22-9-8-20(15-23(22)36-3)34-12-10-33(2)11-13-34/h4-9,14-15,17H,1,10-13,16H2,2-3H3,(H,30,35)(H2,28,29,31,32)
InChi Key UGXCBYVBIJACEK-UHFFFAOYSA-N
Smiles CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NCC4=CC(=CC=C4)NC(=O)C=C)Cl)OC
Isomeric SMILES CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NCC4=CC(=CC=C4)NC(=O)C=C)Cl)OC
PubChem CID 92042864
分子量 508.02

化学和物理性质

溶解性 DMSO : 100 mg/mL (196.84 mM; Need ultrasonic)
分子量 508.000 g/mol
XLogP3 4.200
氢键供体数Hydrogen Bond Donor Count 3
氢键受体数Hydrogen Bond Acceptor Count 8
可旋转键计数Rotatable Bond Count 9
精确质量Exact Mass 507.215 Da
单同位素质量Monoisotopic Mass 507.215 Da
拓扑极表面积Topological Polar Surface Area 94.700 Ų
重原子数Heavy Atom Count 36
形式电荷Formal Charge 0
复杂度Complexity 708.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

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