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依鲁替尼 (PCI-32765)

高效，不可逆的BTK \ xa0抑制剂
规格或纯度: ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
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BLK proto-oncogene，Src family tyrosine kinase Inhibitor BMX non-receptor tyrosine kinase Inhibitor Bruton tyrosine kinase Inhibitor epidermal growth factor receptor Inhibitor erb-b2 receptor tyrosine kinase 2 Inhibitor erb-b2 receptor tyrosine kinase 4 Inhibitor FYN proto-oncogene，Src family tyrosine kinase Inhibitor HCK proto-oncogene，Src family tyrosine kinase Inhibitor IL2 inducible T cell kinase Inhibitor Janus kinase 3 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 tec protein tyrosine kinase Inhibitor TXK tyrosine kinase Inhibitor YES proto-oncogene 1，Src family tyrosine kinase Inhibitor
main product photo

基本描述

规格或纯度 ≥98%
英文名称 Ibrutinib (PCI-32765)
别名 PCI32765;依鲁替尼
英文别名 Ibrutinib;PCI32765;PCI 32765;1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one;CRA-032765;2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide
生化机理 PCI-32765 is a high potent irreversible BTK inhibitor with an IC50 of 0.46 nM for the purified Btk.Highly potent, irreversible Bruton tyrosine kinase (BTK)\xa0inhibitor (IC 50 = 0.5nM). Inhibits autophosphorylation of BTK IC 50 = 11 nM), and phophorylation of PLCγ (IC 50 = 29 nM) and ERK (IC 50 = 13 nM).\xa0 Potently inhbits BLK, BMS, FGR, EGFR and ITK
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 10mg、50mg卖完停产，不再备货；有毒，请参阅SDS以获取更多信息。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

Ibrutinib (PCI-32765)是一种有效的，高选择性的Btk抑制剂，IC50为0.5 nM，作用于Bmx， CSK， FGR， BRK及HCK，适度有效，对EGFR， Yes， ErbB2， JAK3等作用效果稍弱。

Ibrutinib is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

名称和标识符

IUPAC Name 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
INCHI InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1
InChi Key XYFPWWZEPKGCCK-GOSISDBHSA-N
Canonical SMILES C=CC(=O)N1CCCC(C1)N2C3=NC=NC(=C3C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)N
分子式

C25H24N6O2
PubChem CID 24821094
分子量 440.5

化学和物理性质

溶解性 DMSO ≥85mg/mL Water <1.2mg/mL Ethanol ≥1.8mg/mL

安全信息

象形图
ghs08

Health Hazard

ghs09

Environmental Hazard

ghs07

Harmful
信号词 Danger
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H351: Suspected of causing cancer
H373: Causes damage to organs through prolonged or repeated exposure
H302: Harmful if swallowed
H410: Very toxic to aquatic life with long lasting effects
H360: May damage fertility or the unborn child
预防措施声明 P261,P305+P351+P338,P273,P280,P302+P352,P321,P405,P501,P264,P260,P271,P270,P304+P340,P403+P233,P362+P364,P391,P330,P203,P264+P265,P301+P317,P318,P337+P317,P332+P317,P319

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 1799
名称 erb-b2 receptor tyrosine kinase 4
缩写名 HER4
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 1308 2q34 ERBB4 erb-b2 receptor tyrosine kinase 4
Mouse 1 1308 1 33.8 cM Erbb4 erb-b2 receptor tyrosine kinase 4
Rat 1 1308 9q32-q33 Erbb4 erb-b2 receptor tyrosine kinase 4
Ensembl Gene ENSG00000178568 (Hs) , ENSMUSG00000062209 (Mm) , ENSRNOG00000014248 (Rn)
Entrez Gene 13869 (Mm) , 59323 (Rn) , 2066 (Hs)
OMIM 600543 (Hs)
Protein GI 11067415 (Rn) , 146134398 (Mm) , 110825958 (Hs)
UniProtKB Q15303 (Hs) , Q61527 (Mm) , Q62956 (Rn)
RefSeq Nucleotide NM_001042599 (Hs) , NM_010154 (Mm) , NM_021687 (Rn)
RefSeq Protein NP_001036064 (Hs) , NP_034284 (Mm) , NP_067719 (Rn)
Orphanet 370064 (Hs)
DrugBank Target Q15303 (Hs)
CATH/Gene3D 3.80.20.20 (N/A)
ChEMBL Target CHEMBL3009 (Hs)
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 1942
名称 BMX non-receptor tyrosine kinase
缩写名 Etk
家族 Tec family
别名 FFA3R
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 675 Xp22.2 BMX BMX non-receptor tyrosine kinase
Mouse 2 651 X F5 Bmx BMX non-receptor tyrosine kinase
Rat 2 655 X q21 Bmx BMX non-receptor tyrosine kinase
Ensembl Gene ENSG00000102010 (Hs) , ENSMUSG00000031377 (Mm) , ENSRNOG00000003705 (Rn)
Entrez Gene 660 (Hs) , 12169 (Mm) , 367786 (Rn)
OMIM 300101 (Hs)
UniProtKB P51813 (Hs) , P97504 (Mm)
RefSeq Nucleotide NM_001109016 (Rn) , NM_001721 (Hs) , NM_009759 (Mm)
RefSeq Protein NP_001102486 (Rn) , NP_001712 (Hs) , NP_033889 (Mm)
Protein GI 4502435 (Hs) , 226693402 (Mm) , 157824055 (Rn)
CATH/Gene3D 2.30.29.30 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL3834 (Hs) , CHEMBL2034793 (Mm)
Target ID 1948
名称 Bruton tyrosine kinase
缩写名 Btk
家族 Tec family
别名 FFA3R
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 659 Xq22.1 BTK Bruton tyrosine kinase
Mouse 2 659 X 56.18 cM Btk Bruton agammaglobulinemia tyrosine kinase
Rat 2 660 X q34 Btk Bruton tyrosine kinase
Ensembl Gene ENSG00000010671 (Hs) , ENSMUSG00000031264 (Mm) , ENSRNOG00000052407 (Rn)
Entrez Gene 695 (Hs) , 12229 (Mm) , 367901 (Rn)
OMIM 300300 (Hs)
UniProtKB P35991 (Mm) , Q06187 (Hs)
RefSeq Nucleotide NM_000061 (Hs) , NM_001007798 (Rn) , NM_013482 (Mm)
RefSeq Protein NP_000052 (Hs) , NP_001007799 (Rn) , NP_038510 (Mm)
Orphanet 119094 (Hs)
Protein GI 4557377 (Hs) , 161016839 (Mm) , 56119141 (Rn)
CATH/Gene3D 2.30.29.30 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL3259478 (Mm) , CHEMBL5251 (Hs)
Target ID 2019
名称 erb-b2 receptor tyrosine kinase 2
缩写名 HER2
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 1255 17q12 ERBB2 erb-b2 receptor tyrosine kinase 2
Mouse 1 1256 11 D Erbb2 erb-b2 receptor tyrosine kinase 2
Rat 1 1257 10q31 Erbb2 erb-b2 receptor tyrosine kinase 2
Ensembl Gene ENSG00000141736 (Hs) , ENSMUSG00000062312 (Mm) , ENSRNOG00000006450 (Rn)
Entrez Gene 2064 (Hs) , 13866 (Mm) , 24337 (Rn)
OMIM 164870 (Hs)
UniProtKB P04626 (Hs) , P06494 (Rn) , P70424 (Mm)
RefSeq Nucleotide NM_001005862 (Hs) , NM_010194 (Mm) , NM_017003 (Rn)
RefSeq Protein NP_001005862 (Hs) , NP_034324 (Mm) , NP_058699 (Rn)
Protein GI 111185914 (Mm) , 77020289 (Rn) , 54792098 (Hs)
DrugBank Target P04626 (Hs)
CATH/Gene3D 3.80.20.20 (N/A)
ChEMBL Target CHEMBL3848 (Rn) , CHEMBL2311234 (Mm) , CHEMBL1824 (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 2046
名称 IL2 inducible T cell kinase
缩写名 ITK
家族 Tec family
别名 FFA3R
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 620 5q33.3 ITK IL2 inducible T cell kinase
Mouse 2 625 11 B1.1 Itk IL2 inducible T cell kinase
Rat 2 626 10 q21 Itk IL2-inducible T-cell kinase
Ensembl Gene ENSG00000113263 (Hs) , ENSMUSG00000020395 (Mm) , ENSRNOG00000006860 (Rn)
Entrez Gene 3702 (Hs) , 16428 (Mm) , 363577 (Rn)
OMIM 186973 (Hs)
UniProtKB Q03526 (Mm) , Q08881 (Hs)
RefSeq Nucleotide NM_001108825 (Rn) , NM_005546 (Hs) , NM_010583 (Mm)
RefSeq Protein NP_001102295 (Rn) , NP_005537 (Hs) , NP_034713 (Mm)
Orphanet 244711 (Hs)
Protein GI 15718680 (Hs) , 119703751 (Mm) , 157818821 (Rn)
CATH/Gene3D 2.30.29.30 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL2959 (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)
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 2238
名称 tec protein tyrosine kinase
缩写名 TEC
家族 Tec family
别名 FFA3R
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 631 4p12-p11 TEC tec protein tyrosine kinase
Mouse 2 630 5 38.44 cM Tec tec protein tyrosine kinase
Rat 2 629 14 p11 Tec tec protein tyrosine kinase
Ensembl Gene ENSG00000135605 (Hs) , ENSMUSG00000029217 (Mm) , ENSRNOG00000002278 (Rn)
Entrez Gene 7006 (Hs) , 21682 (Mm) , 84492 (Rn)
OMIM 600583 (Hs)
UniProtKB P24604 (Mm) , P42680 (Hs)
RefSeq Nucleotide NM_001113460 (Mm) , NM_003215 (Hs) , NM_053432 (Rn)
RefSeq Protein NP_001106931 (Mm) , NP_003206 (Hs) , NP_445884 (Rn)
Protein GI 130977759 (Hs) , 164698390 (Mm) , 197304782 (Rn)
CATH/Gene3D 2.30.29.30 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL4246 (Hs)
Target ID 2268
名称 TXK tyrosine kinase
缩写名 TXK
家族 Tec family
别名 FFA3R
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 527 4p12 TXK TXK tyrosine kinase
Mouse 2 527 5 38.44 cM Txk TXK tyrosine kinase
Rat 2 526 14 p11 Txk TXK tyrosine kinase
Ensembl Gene ENSG00000074966 (Hs) , ENSMUSG00000054892 (Mm) , ENSRNOG00000025925 (Rn)
Entrez Gene 7294 (Hs) , 22165 (Mm) , 305311 (Rn)
OMIM 600058 (Hs)
UniProtKB P42681 (Hs) , P42682 (Mm)
RefSeq Nucleotide NM_001024255 (Rn) , NM_001122754 (Mm) , NM_003328 (Hs)
RefSeq Protein NP_001019426 (Rn) , NP_001116226 (Mm) , NP_003319 (Hs)
Protein GI 148596974 (Hs) , 170295811 (Mm) , 66730395 (Rn)
CATH/Gene3D 3.30.505.10 (N/A)
ChEMBL Target CHEMBL4367 (Hs)
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 6912
名称 ibrutinib
别名 Imbruvica®
类别 Synthetic organic
学名 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
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 Ibrutinib is a clinically used inhibitor of Bruton's tyrosine kinase. It was originally approved with breakthrough therapy designation through the FDA's accelerated approval program.

参考文献

1. Byrd JC, Furman RR, Coutre SE, Flinn IW, Burger JA, Blum KA, Grant B, Sharman JP, Coleman M, Wierda WG et al..  (2013)  Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia..  N Engl J Med,  369  (1):  (32-42).  [PMID:23782158]
2. Fukasawa T et al..  (2021)  Single-cell-level protein analysis revealing the roles of autoantigen-reactive B lymphocytes in autoimmune disease and the murine model..  Elife,  10  ():  ().  [PMID:34854378]

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