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eCF506

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货号 (SKU) 包装规格 是否现货 价格 数量
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ABL proto-oncogene 1，non-receptor tyrosine kinase Inhibitor BLK proto-oncogene，Src family tyrosine kinase Inhibitor FGR proto-oncogene，Src family tyrosine kinase Inhibitor FYN proto-oncogene，Src family tyrosine kinase Inhibitor fyn related Src family tyrosine kinase Inhibitor HCK proto-oncogene，Src family tyrosine kinase Inhibitor LCK proto-oncogene，Src family tyrosine kinase Inhibitor LYN proto-oncogene，Src family tyrosine kinase Inhibitor SRC proto-oncogene，non-receptor tyrosine kinase Inhibitor YES proto-oncogene 1，Src family tyrosine kinase Inhibitor
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基本描述

英文名称 eCF506
别名 derivative 11a
英文别名 derivative 11a

名称和标识符

IUPAC Name tert-butyl N-[4-(4-amino-1-{2-[4-(dimethylamino)piperidin-1-yl]ethyl}-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl]carbamate
INCHI InChI=1S/C26H38N8O3/c1-26(2,3)37-25(35)30-19-8-7-17(15-20(19)36-6)22-21-23(27)28-16-29-24(21)34(31-22)14-13-33-11-9-18(10-12-33)32(4)5/h7-8,15-16,18H,9-14H2,1-6H3,(H,30,35)(H2,27,28,29)
InChi Key GMPQGWXPDRNCBL-UHFFFAOYSA-N
Canonical SMILES COc1cc(ccc1NC(=O)OC(C)(C)C)c1nn(c2c1c(N)ncn2)CCN1CCC(CC1)N(C)C
PubChem CID 121231408

靶标

Target ID 1923
名称 ABL proto-oncogene 1, non-receptor tyrosine kinase
缩写名 Abl
家族 Abl family
别名 LEC2
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1130 9q34.12 ABL1 ABL proto-oncogene 1, non-receptor tyrosine kinase
Mouse 2 1123 2 B Abl1 c-abl oncogene 1, non-receptor tyrosine kinase
Rat 2 1143 3p12 Abl1 ABL proto-oncogene 1, non-receptor tyrosine kinase
Ensembl Gene ENSG00000097007 (Hs) , ENSMUSG00000026842 (Mm) , ENSRNOG00000047356 (Rn)
Entrez Gene 25 (Hs) , 11350 (Mm) , 311860 (Rn)
OMIM 189980 (Hs)
UniProtKB P00519 (Hs) , P00520 (Mm)
RefSeq Nucleotide NM_001100850 (Rn) , NM_001112703 (Mm) , NM_005157 (Hs)
RefSeq Protein NP_001094320 (Rn) , NP_001106174 (Mm) , NP_005148 (Hs)
Orphanet 117691 (Hs)
Protein GI 62362414 (Hs) , 162951870 (Mm) , 291167784 (Rn)
DrugBank Target P00519 (Hs)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL1862 (Hs) , CHEMBL3099 (Mm)
Target ID 1940
名称 BLK proto-oncogene, Src family tyrosine kinase
缩写名 Blk
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 505 8p23.1 BLK BLK proto-oncogene, Src family tyrosine kinase
Mouse 2 499 14 33.25 cM Blk B lymphoid kinase
Rat 2 499 15p12 Blk BLK proto-oncogene, Src family tyrosine kinase
Ensembl Gene ENSG00000136573 (Hs) , ENSMUSG00000014453 (Mm) , ENSRNOG00000010798 (Rn)
Entrez Gene 640 (Hs) , 12143 (Mm) , 364403 (Rn)
OMIM 191305 (Hs)
UniProtKB P16277 (Mm) , P51451 (Hs)
RefSeq Nucleotide NM_001025751 (Rn) , NM_001715 (Hs) , NM_007549 (Mm)
RefSeq Protein NP_001020922 (Rn) , NP_001706 (Hs) , NP_031575 (Mm)
Orphanet 227384 (Hs)
Protein GI 33469982 (Hs) , 31982490 (Mm) , 71043712 (Rn)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL2250 (Hs) , CHEMBL3343 (Mm)
Target ID 2024
名称 FGR proto-oncogene, Src family tyrosine kinase
缩写名 Fgr
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 529 1p35.3 FGR FGR proto-oncogene, Src family tyrosine kinase
Mouse 2 517 4 D2.3 Fgr FGR proto-oncogene, Src family tyrosine kinase
Rat 2 517 5q36 Fgr FGR proto-oncogene, Src family tyrosine kinase
Ensembl Gene ENSG00000000938 (Hs) , ENSMUSG00000028874 (Mm) , ENSRNOG00000009912 (Rn)
Entrez Gene 2268 (Hs) , 14191 (Mm) , 79113 (Rn)
OMIM 164940 (Hs)
UniProtKB P09769 (Hs) , P14234 (Mm) , Q6P6U0 (Rn)
RefSeq Nucleotide NM_001042729 (Hs) , NM_010208 (Mm) , NM_024145 (Rn)
RefSeq Protein NP_001036194 (Hs) , NP_034338 (Mm) , NP_077059 (Rn)
Protein GI 112382241 (Hs) , 171542819 (Mm) , 40254761 (Rn)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL4362 (Rn) , CHEMBL2034795 (Mm) , CHEMBL4454 (Hs)
Target ID 2025
名称 fyn related Src family tyrosine kinase
缩写名 FRK
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 505 6q22.1 FRK fyn related Src family tyrosine kinase
Mouse 2 512 10 B1 Frk fyn-related kinase
Rat 2 506 20q12 Frk fyn-related Src family tyrosine kinase
Ensembl Gene ENSG00000111816 (Hs) , ENSMUSG00000019779 (Mm) , ENSRNOG00000000543 (Rn)
Entrez Gene 2444 (Hs) , 14302 (Mm) , 79209 (Rn)
OMIM 606573 (Hs)
UniProtKB P42685 (Hs) , Q62662 (Rn) , Q922K9 (Mm)
RefSeq Nucleotide NM_001159544 (Mm) , NM_002031 (Hs) , NM_024368 (Rn)
RefSeq Protein NP_001153016 (Mm) , NP_002022 (Hs) , NP_077344 (Rn)
Protein GI 4503787 (Hs) , 227116298 (Mm) , 13242263 (Rn)
DrugBank Target P42685 (Hs)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL4223 (Hs)
Target ID 2026
名称 FYN proto-oncogene, Src family tyrosine kinase
缩写名 Fyn
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 537 6q21 FYN FYN proto-oncogene, Src family tyrosine kinase
Mouse 2 537 10 20.51 cM Fyn Fyn proto-oncogene
Rat 2 537 20q12 Fyn FYN proto-oncogene, Src family tyrosine kinase
Ensembl Gene ENSG00000010810 (Hs) , ENSMUSG00000019843 (Mm) , ENSRNOG00000000596 (Rn)
Entrez Gene 2534 (Hs) , 14360 (Mm) , 25150 (Rn)
OMIM 137025 (Hs)
UniProtKB P06241 (Hs) , P39688 (Mm) , Q62844 (Rn)
RefSeq Nucleotide NM_001122892 (Mm) , NM_002037 (Hs) , NM_012755 (Rn)
RefSeq Protein NP_001116364 (Mm) , NP_002028 (Hs) , NP_036887 (Rn)
Protein GI 4503823 (Hs) , 171543839 (Mm) , 6978863 (Rn)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL1841 (Hs) , CHEMBL4517 (Mm)
Target ID 2032
名称 HCK proto-oncogene, Src family tyrosine kinase
缩写名 Hck
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 526 20q11.21 HCK HCK proto-oncogene, Src family tyrosine kinase
Mouse 2 524 2 75.41 cM Hck hemopoietic cell kinase
Rat 2 524 3q41 Hck HCK proto-oncogene, Src family tyrosine kinase
Ensembl Gene ENSG00000101336 (Hs) , ENSMUSG00000003283 (Mm) , ENSRNOG00000009331 (Rn)
Entrez Gene 3055 (Hs) , 15162 (Mm) , 25734 (Rn)
OMIM 142370 (Hs)
UniProtKB P08103 (Mm) , P08631 (Hs) , P50545 (Rn)
RefSeq Nucleotide NM_001172129 (Hs) , NM_010407 (Mm) , NM_013185 (Rn)
RefSeq Protein NP_002101 (Hs) , NP_034537 (Mm) , NP_037317 (Rn)
Protein GI 30795229 (Hs) , 34734056 (Mm) , 34734058 (Rn)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL3234 (Hs)
Target ID 2053
名称 LCK proto-oncogene, Src family tyrosine kinase
缩写名 Lck
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 509 1p35.2 LCK LCK proto-oncogene, Src family tyrosine kinase
Mouse 2 509 4 63.26 cM Lck lymphocyte protein tyrosine kinase
Rat 2 509 5q36 Lck LCK proto-oncogene, Src family tyrosine kinase
Ensembl Gene ENSG00000182866 (Hs) , ENSMUSG00000000409 (Mm) , ENSRNOG00000009705 (Rn)
Entrez Gene 3932 (Hs) , 16818 (Mm) , 313050 (Rn)
OMIM 153390 (Hs)
UniProtKB P06239 (Hs) , P06240 (Mm) , Q01621 (Rn)
RefSeq Nucleotide NM_001042771 (Hs) , NM_001100709 (Rn) , NM_001162432 (Mm)
RefSeq Protein NP_001036236 (Hs) , NP_001094179 (Rn) , NP_001155904 (Mm)
Orphanet 280151 (Hs)
Protein GI 112789548 (Hs) , 244791455 (Mm) , 189181659 (Rn)
DrugBank Target P06239 (Hs)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL258 (Hs) , CHEMBL2480 (Mm)
Target ID 2060
名称 LYN proto-oncogene, Src family tyrosine kinase
缩写名 Lyn
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 512 8q12.1 LYN LYN proto-oncogene, Src family tyrosine kinase
Mouse 2 512 4 2.05 cM Lyn LYN proto-oncogene, Src family tyrosine kinase
Rat 2 512 5q12 Lyn LYN proto-oncogene, Src family tyrosine kinase
Ensembl Gene ENSG00000254087 (Hs) , ENSMUSG00000042228 (Mm) , ENSRNOG00000008180 (Rn)
Entrez Gene 4067 (Hs) , 17096 (Mm) , 81515 (Rn)
OMIM 165120 (Hs)
UniProtKB P07948 (Hs) , P25911 (Mm) , Q07014 (Rn)
RefSeq Nucleotide NM_001111097 (Hs) , NM_002350 (Mm) , NM_030857 (Rn) , NM_001111098 (Hs) , NM_001111098 (Rn) , NM_010747 (Mm)
RefSeq Protein NP_001104566 (Mm) , NP_002341 (Hs) , NP_110484 (Rn) , NP_001104567 (Hs) , NP_001104568 (Rn) , NP_034877 (Mm)
Protein GI 162287326 (Hs) , 4505055 (Hs) , 161760636 (Mm) , 161760634 (Mm) , 161760646 (Rn) , 13540677 (Rn)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL4363 (Rn) , CHEMBL3905 (Hs) , CHEMBL2258 (Mm)
Target ID 2206
名称 SRC proto-oncogene, non-receptor tyrosine kinase
缩写名 Src
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 536 20q11.23 SRC SRC proto-oncogene, non-receptor tyrosine kinase
Mouse 2 541 2 78.35 cM Src Rous sarcoma oncogene
Rat 2 536 3q42 Src SRC proto-oncogene, non-receptor tyrosine kinase
Ensembl Gene ENSG00000197122 (Hs) , ENSMUSG00000027646 (Mm) , ENSRNOG00000009495 (Rn)
Entrez Gene 6714 (Hs) , 20779 (Mm) , 83805 (Rn)
OMIM 190090 (Hs)
UniProtKB P05480 (Mm) , P12931 (Hs) , Q9WUD9 (Rn)
RefSeq Nucleotide NM_001025395 (Mm) , NM_005417 (Hs) , NM_031977 (Rn)
RefSeq Protein NP_001020566 (Mm) , NP_005408 (Hs) , NP_114183 (Rn)
Protein GI 4885609 (Hs) , 70794809 (Mm) , 14010835 (Rn)
DrugBank Target P12931 (Hs)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL267 (Hs) , CHEMBL3074 (Mm) , CHEMBL3014 (Rn)
Target ID 2284
名称 YES proto-oncogene 1, Src family tyrosine kinase
缩写名 Yes
家族 Src family
别名 RMLP-R-I
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 543 18p11.32 YES1 YES proto-oncogene 1, Src family tyrosine kinase
Mouse 2 541 5 17.33 cM Yes1 YES proto-oncogene 1, Src family tyrosine kinase
Rat 2 541 9q38 Yes1 YES proto-oncogene 1, Src family tyrosine kinase
Ensembl Gene ENSG00000176105 (Hs) , ENSMUSG00000014932 (Mm) , ENSRNOG00000037227 (Rn)
Entrez Gene 7525 (Hs) , 22612 (Mm) , 24884 (Rn)
OMIM 164880 (Hs)
UniProtKB F1LM93 (Rn) , P07947 (Hs) , Q04736 (Mm)
RefSeq Nucleotide NM_001205132 (Mm) , NM_005433 (Hs) , NM_033298 (Rn)
RefSeq Protein NP_001192061 (Mm) , NP_005424 (Hs) , NP_150640 (Rn)
Protein GI 4885661 (Hs) , 326806986 (Mm) , 51491819 (Rn)
DrugBank Target P07947 (Hs)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL2073 (Hs)

关联配体

Ligand ID 9186
名称 eCF506
别名 derivative 11a [PMID: 27115835]
类别 Synthetic organic
学名 tert-butyl N-[4-(4-amino-1-{2-[4-(dimethylamino)piperidin-1-yl]ethyl}-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl]carbamate
生物活性评价 eCF506 is >950-fold selective for SRC kinases over ABL kinase . IC50s for inhibition of the receptor tyrosine kinases KIT, mTOR, PDGFRα and RET are all >1000 nM .
评价 eCF506 is a potent and selective inhibitor of SRC family kinases, with activity against breast cancer cells in vitro and in vivo. Design and discovery of this compound is reported in .

参考文献

1. Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC et al..  (2016)  Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase..  J Med Chem,  59  (10):  (4697-710).  [PMID:27115835]

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