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GW2580,cFMS RTK抑制剂

选择性cFMS RTK抑制剂。细胞可渗透的。
规格或纯度: ≥99%
有货

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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
G129822-25mg
25mg 现货 Stock Image
G129822-50mg
50mg 现货 Stock Image
G129822-250mg
250mg 现货 Stock Image
G129822-1g
1g 现货 Stock Image

基本描述

规格或纯度 ≥99%
英文名称 GW2580
别名 5-[[3-甲氧基-4-[(4-甲氧基苯基)甲氧基]苯基]甲基] -2,4-甲苯酚二胺|5-[[3-甲氧基-4-[(4-甲氧基苯基)甲氧基]苯基]甲基]熔融吡啶-2,4-二胺|GW-2580|5-[3-甲氧基-4-[(4-甲氧基苄基)氧]苄基]嘧啶-2,4-二胺
英文别名 870483-87-7|GW2580|GW-2580|5-(3-Methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine|GW632580X|GW 2580|5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine|SRV0JCF9LI|SC-203877|cFMS Receptor Tyrosine Kinase Inhibitor|GW-
生化机理 选择性cFMS(集落刺激因子1)RTK抑制剂。体外抑制单核细胞生长(IC 50 = 0.2μM)和体内LPS诱导的TNF-α产生。抑制中枢神经系统的巨噬细胞浸润。口服具有活性细胞可渗透的。
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

选择性的 c-Fms 激酶抑制剂,体外实验中在 0.06 μM 时可完全抑制人 cFMS 激酶。GW2580 是 ATP 与 cFMS 激酶结合的竞争性抑制剂,并且可以抑制集落刺激因子 1 信号传导。

GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling

名称和标识符

IUPAC Name 5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine
INCHI InChI=1S/C20H22N4O3/c1-25-16-6-3-13(4-7-16)12-27-17-8-5-14(10-18(17)26-2)9-15-11-23-20(22)24-19(15)21/h3-8,10-11H,9,12H2,1-2H3,(H4,21,22,23,24)
InChi Key MYQAUKPBNJWPIE-UHFFFAOYSA-N
Canonical SMILES COC1=CC=C(C=C1)COC2=C(C=C(C=C2)CC3=CN=C(N=C3N)N)OC
分子式

C20H22N4O3

PubChem CID 11617559
分子量 366.41

化学和物理性质

溶解性 DMSO 48 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
敏感性 对热敏感

安全信息

象形图
ghs07

Harmful

信号词 Warning
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H302: Harmful 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+P317,P337+P317,P332+P317,P319
WGK Germany 3

靶标

Target ID 1806
名称 colony stimulating factor 1 receptor
缩写名 CSFR
家族 Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family
别名 mrgG
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 972 5q32 CSF1R colony stimulating factor 1 receptor
Mouse 1 977 18 34.41 cM Csf1r colony stimulating factor 1 receptor
Rat 1 978 18q12.1 Csf1r colony stimulating factor 1 receptor
Ensembl Gene ENSG00000182578 (Hs) , ENSMUSG00000024621 (Mm) , ENSRNOG00000018414 (Rn)
Entrez Gene 12978 (Mm) , 307403 (Rn) , 1436 (Hs)
OMIM 164770 (Hs)
Protein GI 71361659 (Rn) , 27262659 (Hs) , 126723423 (Mm)
UniProtKB P07333 (Hs) , P09581 (Mm) , Q00495 (Rn)
RefSeq Nucleotide NM_001029901 (Rn) , NM_001037859 (Mm) , NM_005211 (Hs)
RefSeq Protein NP_001025072 (Rn) , NP_001032948 (Mm) , NP_005202 (Hs)
Orphanet 317674 (Hs)
CATH/Gene3D 2.60.40.10 (N/A)
ChEMBL Target CHEMBL1844 (Hs) , CHEMBL5570 (Mm)
Target ID 1817
名称 neurotrophic receptor tyrosine kinase 1
缩写名 trkA
家族 Type VII RTKs: Neurotrophin receptor/Trk family
别名 Sensory neuron-specific G-protein coupled receptor 4
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 796 1q23.1 NTRK1 neurotrophic receptor tyrosine kinase 1
Mouse 1 799 3 38.62 cM Ntrk1 neurotrophic tyrosine kinase, receptor, type 1
Rat 1 799 2q34 Ntrk1 neurotrophic receptor tyrosine kinase 1
Ensembl Gene ENSG00000198400 (Hs) , ENSMUSG00000028072 (Mm) , ENSRNOG00000013953 (Rn)
Entrez Gene 18211 (Mm) , 59109 (Rn) , 4914 (Hs)
OMIM 191315 (Hs)
Protein GI 11024666 (Rn) , 59889558 (Hs) , 169234626 (Mm)
UniProtKB P04629 (Hs) , P35739 (Rn) , Q3UFB7 (Mm)
RefSeq Nucleotide NM_001007792 (Hs) , NM_001033124 (Mm) , NM_021589 (Rn)
RefSeq Protein NP_001007793 (Hs) , NP_001028296 (Mm) , NP_067600 (Rn)
Orphanet 123961 (Hs)
DrugBank Target P04629 (Hs)
CATH/Gene3D 2.60.40.10 (N/A) , 3.80.10.10 (N/A)
ChEMBL Target CHEMBL2815 (Hs) , CHEMBL4220 (Rn)
Target ID 1818
名称 neurotrophic receptor tyrosine kinase 2
缩写名 trkB
家族 Type VII RTKs: Neurotrophin receptor/Trk family
别名 Sensory neuron-specific G-protein coupled receptor 4
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 822 9q21.33 NTRK2 neurotrophic receptor tyrosine kinase 2
Mouse 1 821 13 31.2 cM Ntrk2 neurotrophic tyrosine kinase, receptor, type 2
Rat 1 821 17p14 Ntrk2 neurotrophic receptor tyrosine kinase 2
Ensembl Gene ENSG00000148053 (Hs) , ENSMUSG00000055254 (Mm) , ENSRNOG00000018839 (Rn)
Entrez Gene 18212 (Mm) , 25054 (Rn) , 4915 (Hs)
OMIM 600456 (Hs)
Protein GI 65506779 (Hs) , 253683490 (Rn) , 68215970 (Mm)
UniProtKB P15209 (Mm) , Q16620 (Hs) , Q63604 (Rn)
RefSeq Nucleotide NM_001007097 (Hs) , NM_001025074 (Mm) , NM_001163168 (Rn)
RefSeq Protein NP_001007098 (Hs) , NP_001020245 (Mm) , NP_032771 (Mm) , NP_036863 (Rn)
Orphanet 363263 (Hs)
CATH/Gene3D 2.60.40.10 (N/A) , 3.80.10.10 (N/A)
ChEMBL Target CHEMBL4523190 (Mm) , CHEMBL1795111 (Rn) , CHEMBL4898 (Hs)
Target ID 1819
名称 neurotrophic receptor tyrosine kinase 3
缩写名 trkC
家族 Type VII RTKs: Neurotrophin receptor/Trk family
别名 Sensory neuron-specific G-protein coupled receptor 4
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 839 15q25.3 NTRK3 neurotrophic receptor tyrosine kinase 3
Mouse 1 825 7 44.01 cM Ntrk3 neurotrophic tyrosine kinase, receptor, type 3
Rat 1 864 1q31 Ntrk3 neurotrophic receptor tyrosine kinase 3
Ensembl Gene ENSG00000140538 (Hs) , ENSMUSG00000059146 (Mm) , ENSRNOG00000018674 (Rn)
Entrez Gene 18213 (Mm) , 29613 (Rn) , 4916 (Hs)
OMIM 191316 (Hs)
Protein GI 33413429 (Mm) , 340745353 (Hs) , 9506939 (Rn)
UniProtKB Q03351 (Rn) , Q16288 (Hs) , Q6VNS1 (Mm)
RefSeq Nucleotide NM_001007156 (Hs) , NM_001270656 (Rn) , NM_008746 (Mm)
RefSeq Protein NP_001007157 (Hs) , NP_001257585 (Rn) , NP_032772 (Mm) , NP_877961 (Mm)
Orphanet 246681 (Hs)
CATH/Gene3D 2.60.40.10 (N/A) , 3.80.10.10 (N/A)
ChEMBL Target CHEMBL5608 (Hs) , CHEMBL2791 (Mm)

关联配体

Ligand ID 5685
名称 GW-2580
别名 GW2580
类别 Synthetic organic
学名 5-({3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl}methyl)pyrimidine-2,4-diamine
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 GW-2580 is an inhibitor of the receptor tyrosine kinase, colony stimulating factor 1 receptor (CSF1R or FMS) . CSF1R inhibitors are considered to have therapeutic potential for the prevention of osteolytic disease associated with bone metastasis and other bone diseases. GW-2580 has been assessed in preclinical investigations.

参考文献

1. Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM et al..  (2005)  Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580..  Proc Natl Acad Sci USA,  102  (44):  (16078-83).  [PMID:16249345]
2. Baghdadi M et al..  (2016)  Chemotherapy-Induced IL34 Enhances Immunosuppression by Tumor-Associated Macrophages and Mediates Survival of Chemoresistant Lung Cancer Cells..  Cancer Res,  76  (20):  (6030-6042).  [PMID:27550451]

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