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托法替尼

强大的细胞渗透性\ xa0Janus激酶（JAK）抑制剂
规格或纯度: ≥98% (HPLC)
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Janus kinase 1 Inhibitor Janus kinase 2 Inhibitor Janus kinase 3 Inhibitor protein kinase N1 Inhibitor tyrosine kinase 2 Inhibitor
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基本描述

规格或纯度 ≥98% (HPLC)
英文名称 Tofacitinib
别名 (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate salt 3-[(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]- 3-oxopropanenitrile citrate salt CP-690550-10 Tasocitinib
英文别名 (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate salt 3-[(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]- 3-oxopropanenitrile citrate salt CP-690550-10 Tasocitinib
生化机理 托法替尼(Tofacitinib) 是一种强效Janus激酶3（JAK3）抑制剂，而且还带有一些JAK-1抑制活性。它会阻止下游STAT信号导致强效抑制炎性细胞因子产生的免疫抑制和抗炎活性。托法替尼(Tofacitinib)正在研究用于一些自身免疫性疾病包括类风湿关节炎，银屑病和干眼症的治疗。具有某些JAK1抑制活性的有力的，细胞可渗透的詹纳斯激酶3（JAK3）抑制剂。吡咯并[2,3-d]嘧啶衍生物。阻断下游STAT信号传导，从而有效抑制炎症因子并产生免疫抑制。
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。

名称和标识符

IUPAC Name 3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
INCHI InChI=1S/C16H20N6O/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/m1/s1
InChi Key UJLAWZDWDVHWOW-YPMHNXCESA-N
Canonical SMILES CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
分子式

C16H20N6O
PubChem CID 9926791
分子量 312.37

安全信息

象形图
ghs06

Toxic

ghs08

Health 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
H301: Toxic if swallowed
H311: Toxic in contact with skin
H331: Toxic if inhaled
H351: Suspected of causing cancer
H373: Causes damage to organs through prolonged or repeated exposure
H302: Harmful if swallowed
H360: May damage fertility or the unborn child
H360Df: May damage the unborn child; Suspected of damaging fertility
预防措施声明 P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P260,P271,P270,P304+P340,P403+P233,P362+P364,P330,P361+P364,P203,P264+P265,P301+P316,P301+P317,P318,P337+P317,P332+P317,P316,P319
WGK Germany 3

靶标

Target ID 1520
名称 protein kinase N1
缩写名 PKN1
家族 Protein kinase N (PKN) family
别名 MGC99678
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 942 19p13.12 PKN1 protein kinase N1
Mouse 2 946 8 40.22 cM Pkn1 protein kinase N1
Rat 2 946 19q11 Pkn1 protein kinase N1
Ensembl Gene ENSG00000123143 (Hs) , ENSMUSG00000057672 (Mm) , ENSRNOG00000004131 (Rn)
Entrez Gene 320795 (Mm) , 29355 (Rn) , 5585 (Hs)
OMIM 601032 (Hs)
Protein GI 47132591 (Hs) , 313760674 (Mm) , 166063985 (Rn)
UniProtKB P70268 (Mm) , Q16512 (Hs) , Q63433 (Rn)
RefSeq Nucleotide NM_002741 (Hs) , NM_017175 (Rn) , NM_177262 (Mm)
RefSeq Protein NP_001186522 (Mm) , NP_002732 (Hs) , NP_058871 (Rn) , NP_796236 (Mm)
CATH/Gene3D 2.60.40.150 (N/A)
ChEMBL Target CHEMBL3384 (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)
Target ID 2269
名称 tyrosine kinase 2
缩写名 Tyk2
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 1187 19p13.2 TYK2 tyrosine kinase 2
Mouse 2 1184 9 A3 Tyk2 tyrosine kinase 2
Rat 2 1186 8q13 Tyk2 tyrosine kinase 2
Ensembl Gene ENSG00000105397 (Hs) , ENSMUSG00000032175 (Mm) , ENSRNOG00000032948 (Rn)
Entrez Gene 7297 (Hs) , 54721 (Mm) , 100361294 (Rn)
OMIM 176941 (Hs)
UniProtKB P29597 (Hs) , Q9R117 (Mm)
RefSeq Nucleotide NM_001205312 (Mm) , NM_001257347 (Rn) , NM_003331 (Hs)
RefSeq Protein NP_001192241 (Mm) , NP_001244276 (Rn) , NP_003322 (Hs)
Orphanet 159075 (Hs)
Protein GI 187608615 (Hs) , 328887920 (Mm) , 383087738 (Rn)
CATH/Gene3D 1.20.80.10 (N/A) , 3.30.505.10 (N/A)
ChEMBL Target CHEMBL2321619 (Mm) , CHEMBL3553 (Hs)

关联配体

Ligand ID 5677
名称 tofacitinib
别名 CP-690550
类别 Synthetic organic
学名 3-[(3R,4R)-4-methyl-3-[methyl({7H-pyrrolo[2,3-d]pyrimidin-4-yl})amino]piperidin-1-yl]-3-oxopropanenitrile
生物活性评价 Like many first generation kinase inhibitors tofacitinib exhibits a high degree of broad kinome selectivity but is in reality a pan-JAK-inhibitor. Additional kinases inhibited by tofacitinib in biochemical and cellular assays are described in . Tofacitinib is also reported to exhibit immunosuppressive activity which prevents organ rejection in mice and primates .
Despite clinical efficacy in ulcerative colitis, tofacitinib did not show significant efficacy as an induction and maintenance therapy over placebo, in Crohn's disease patients (as evaluated in Phase 2 studies NCT01393626 and NCT01393899) .
评价 Tofacitinib is an orally active, Type-1 Janus kinase (JAK) inhibitor and it was first approved by the US FDA in 2012. Tofacitinib was originally described as a selective JAK3 inhibitor , but subsequent analysis has revealed it to be a pan-JAK inhibitor, with predominant JAK1 inhibition .

参考文献

1. Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH et al..  (2003)  Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor..  Science,  302  (5646):  (875-8).  [PMID:14593182]
2. Flanagan ME, Blumenkopf TA, Brissette WH, Brown MF, Casavant JM, Shang-Poa C, Doty JL, Elliott EA, Fisher MB, Hines M et al..  (2010)  Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection..  J Med Chem,  53  (24):  (8468-84).  [PMID:21105711]
3. Ghoreschi K, Jesson MI, Li X, Lee JL, Ghosh S, Alsup JW, Warner JD, Tanaka M, Steward-Tharp SM, Gadina M et al..  (2011)  Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550)..  J Immunol,  186  (7):  (4234-43).  [PMID:21383241]
4. Panés J, Sandborn WJ, Schreiber S, Sands BE, Vermeire S, D'Haens G, Panaccione R, Higgins PDR, Colombel JF, Feagan BG et al..  (2017)  Tofacitinib for induction and maintenance therapy of Crohn's disease: results of two phase IIb randomised placebo-controlled trials..  Gut,  66  (6):  (1049-1059).  [PMID:28209624]
5. Sandborn WJ, Su C, Sands BE, D'Haens GR, Vermeire S, Schreiber S, Danese S, Feagan BG, Reinisch W, Niezychowski W et al..  (2017)  Tofacitinib as Induction and Maintenance Therapy for Ulcerative Colitis..  N Engl J Med,  376  (18):  (1723-1736).  [PMID:28467869]
6. Clark JD, Flanagan ME, Telliez JB.  (2014)  Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases..  J Med Chem,  57  (12):  (5023-38).  [PMID:24417533]
7. Kennedy Crispin M, Ko JM, Craiglow BG, Li S, Shankar G, Urban JR, Chen JC, Cerise JE, Jabbari A, Winge MC et al..  (2016)  Safety and efficacy of the JAK inhibitor tofacitinib citrate in patients with alopecia areata..  JCI Insight,  1  (15):  (e89776).  [PMID:27699252]
8. Ostrovskyi D, Rumpf T, Eib J, Lumbroso A, Slynko I, Klaeger S, Heinzlmeir S, Forster M, Gehringer M, Pfaffenrot E et al..  (2016)  Tofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1)..  Future Med Chem,  8  (13):  (1537-51).  [PMID:27572962]
9. Panés J, Vermeire S, Lindsay JO, Sands BE, Su C, Friedman G, Zhang H, Yarlas A, Bayliss M, Maher S et al..  (2018)  Tofacitinib in Patients with Ulcerative Colitis: Health-Related Quality of Life in Phase 3 Randomised Controlled Induction and Maintenance Studies..  J Crohns Colitis,  12  (2):  (145-156).  [PMID:29028981]
10. Motoya S, Watanabe M, Kim HJ, Kim YH, Han DS, Yuasa H, Tabira J, Isogawa N, Arai S, Kawaguchi I et al..  (2018)  Tofacitinib induction and maintenance therapy in East Asian patients with active ulcerative colitis: subgroup analyses from three phase 3 multinational studies..  Intest Res,  16  (2):  (233-245).  [PMID:29743836]

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