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WHI-P154,JAK3激酶抑制剂

JAK3激酶抑制剂。也抑制EGFR
规格或纯度: ≥98%
有货

库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
W125072-10mg 10mg 现货 Stock Image
W125072-50mg 50mg 现货 Stock Image
大包装询价 添加到收藏夹 比较
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epidermal growth factor receptor Inhibitor Janus kinase 1 Inhibitor Janus kinase 2 Inhibitor Janus kinase 3 Inhibitor
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基本描述

规格或纯度 ≥98%
英文名称 WHI-P154
别名 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol;WHI-P 154;4-(3'-Bromo-4'-hydroxyphenyl)amino-6,7-dimethoxyquinazoline
英文别名 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol;WHI-P 154;4-(3'-Bromo-4'-hydroxyphenyl)amino-6,7-dimethoxyquinazoline
生化机理 JAK3抑制剂（IC50 =1.8μM），对JAK1或JAK2无活性。在体外抑制STAT1激活，iNOS表达和NO生成。还抑制其他常见的激酶，包括EGFR（IC50 = 4 nM），Src，Abl，VEGFR，MAPK和PI 3-K，并诱导人胶质母细胞瘤细胞系凋亡（IC50 =158μM）。诱导神经祖细胞分化。
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 50mg卖完停产，不再备货
产品介绍

WHI-P154是一种有效的JAK3抑制剂，IC50为1.8 μM，对JAK1和JAK2没有抑制活性，也抑制EGFR， Src， Abl， VEGFR和MAPK，抑制Stat3而非Stat5磷酸化A JAK3 inhibitor which inhibits other common kinases.

WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.
A JAK3 inhibitor which inhibits other common kinases.

名称和标识符

IUPAC Name 2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
INCHI InChI=1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8,21H,1-2H3,(H,18,19,20)
InChi Key CBIAKDAYHRWZCU-UHFFFAOYSA-N
Canonical SMILES COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)O)Br)OC
分子式

C16H14BrN3O3
PubChem CID 3795
分子量 376.2

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 37.62, 最高浓度(mM): 100
敏感性 对热敏感
熔点 230 °C

安全信息

象形图
ghs06

Toxic

ghs07

Harmful
信号词 Danger
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H301: Toxic if swallowed
预防措施声明 P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P270,P304+P340,P403+P233,P362+P364,P330,P264+P265,P301+P316,P337+P317,P332+P317,P319
WGK Germany 3

靶标

Target ID 1797
名称 epidermal growth factor receptor
缩写名 EGFR
家族 Type I RTKs: ErbB (epidermal growth factor) receptor family
别名 MAS-related GPR, member G
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 1210 7p11.2 EGFR epidermal growth factor receptor
Mouse 1 1210 11 9.41 cM Egfr epidermal growth factor receptor
Rat 2 1209 14q22 Egfr epidermal growth factor receptor
Ensembl Gene ENSG00000146648 (Hs) , ENSMUSG00000020122 (Mm) , ENSRNOG00000004332 (Rn)
Entrez Gene 13649 (Mm) , 24329 (Rn) , 1956 (Hs)
OMIM 131550 (Hs)
Protein GI 46560582 (Mm) , 25742617 (Rn) , 41327736 (Hs)
UniProtKB P00533 (Hs) , Q01279 (Mm)
RefSeq Nucleotide NM_005228 (Hs) , NM_031507 (Rn) , NM_207655 (Mm)
RefSeq Protein NP_005219 (Hs) , NP_031938 (Mm) , NP_113695 (Rn) , NP_997538 (Mm)
Orphanet 121311 (Hs)
DrugBank Target P00533 (Hs)
CATH/Gene3D 3.80.20.20 (N/A)
ChEMBL Target CHEMBL3608 (Mm) , CHEMBL203 (Hs)
Target ID 2047
名称 Janus kinase 1
缩写名 JAK1
家族 Janus kinase (JakA) family
别名 CRF-R1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1154 1p31.3 JAK1 Janus kinase 1
Mouse 2 1153 4 2.05 cM Jak1 Janus kinase 1
Rat 2 1153 5 q31.3-q35 Jak1 Janus kinase 1
Ensembl Gene ENSG00000162434 (Hs) , ENSMUSG00000028530 (Mm) , ENSRNOG00000011157 (Rn)
Entrez Gene 3716 (Hs) , 16451 (Mm) , 84598 (Rn)
OMIM 147795 (Hs)
UniProtKB P23458 (Hs) , P52332 (Mm)
RefSeq Nucleotide NM_002227 (Hs) , NM_053466 (Rn) , NM_146145 (Mm)
RefSeq Protein NP_002218 (Hs) , NP_445918 (Rn) , NP_666257 (Mm)
Protein GI 102469034 (Hs) , 111607496 (Mm) , 197209847 (Rn)
DrugBank Target P23458 (Hs)
CATH/Gene3D 1.20.80.10 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL2835 (Hs) , CHEMBL2968 (Mm)
Target ID 2048
名称 Janus kinase 2
缩写名 JAK2
家族 Janus kinase (JakA) family
别名 CRF-R1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1132 9p24.1 JAK2 Janus kinase 2
Mouse 2 1129 19 23.73 cM Jak2 Janus kinase 2
Rat 2 1132 1q52 Jak2 Janus kinase 2
Ensembl Gene ENSG00000096968 (Hs) , ENSMUSG00000024789 (Mm) , ENSRNOG00000059968 (Rn)
Entrez Gene 3717 (Hs) , 16452 (Mm) , 24514 (Rn)
OMIM 147796 (Hs)
UniProtKB O60674 (Hs) , Q62120 (Mm) , Q62689 (Rn)
RefSeq Nucleotide NM_001048177 (Mm) , NM_004972 (Hs) , NM_031514 (Rn)
RefSeq Protein NP_001041642 (Mm) , NP_004963 (Hs) , NP_113702 (Rn)
Orphanet 122727 (Hs)
Protein GI 4826776 (Hs) , 114326478 (Mm) , 13928696 (Rn)
DrugBank Target O60674 (Hs)
CATH/Gene3D 1.20.80.10 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL1075225 (Rn) , CHEMBL1649049 (Mm) , CHEMBL2971 (Hs)
Target ID 2049
名称 Janus kinase 3
缩写名 JAK3
家族 Janus kinase (JakA) family
别名 CRF-R1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1124 19p13.11 JAK3 Janus kinase 3
Mouse 2 1100 8 34.43 cM Jak3 Janus kinase 3
Rat 2 1100 16p14 Jak3 Janus kinase 3
Ensembl Gene ENSG00000105639 (Hs) , ENSMUSG00000031805 (Mm) , ENSRNOG00000018669 (Rn)
Entrez Gene 3718 (Hs) , 16453 (Mm) , 25326 (Rn)
OMIM 600173 (Hs)
UniProtKB P52333 (Hs) , Q62137 (Mm) , Q63272 (Rn)
RefSeq Nucleotide NM_000215 (Hs) , NM_001190830 (Mm) , NM_012855 (Rn)
RefSeq Protein NP_000206 (Hs) , NP_001177759 (Mm) , NP_036987 (Rn)
Orphanet 122729 (Hs)
Protein GI 47157315 (Hs) , 300192999 (Mm) , 300116243 (Rn)
DrugBank Target P52333 (Hs)
CATH/Gene3D 1.20.80.10 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL2148 (Hs) , CHEMBL4295857 (Rn) , CHEMBL5250 (Mm)

关联配体

Ligand ID 5993
名称 JAK3 inhibitor II
别名 WHI-P154
类别 Synthetic organic
学名 2-bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Sulfadimidine (sulfamethazine) is a sulfonamide antibacterial compound. This class of compounds are competitive inhibitors of bacterial dihydropteroate synthase (DHPS), an enzyme in the pathway which generates the folic acid that is essential for bacterial growth.

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