MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Tofacitinib citrate

CAS No. : 540737-29-9

MCE 国际站：Tofacitinib citrate

产品活性：Tofacitinib citrate是 JAK3/2/1 抑制剂，IC₅₀ 分别为1，20 和 112 nM。Tofacitinib citrate 具有抗菌，抗真菌和抗病毒活性。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt  |  Apoptosis  |  Anti-infection

作用靶点：JAK  |  Apoptosis  |  Bacterial  |  Fungal  |  Influenza Virus

In Vitro: Tofacitinib (CP-690550) citrate binds potentially at JAK3 and JAK2 as 2.2 nM and 5 nM (K_d). The report includes additional binding for Tofacitinib at Camk1 (K_d of 5,000 nM), DCamkL3 (K_d of 4.5 nM), Mst2 (K_d of 4,300 nM), Pkn1 (K_d of 200 nM), Rps6ka2 (Kin.Dom.2-C-terminal) (K_d of 1,400 nM), Rps6ka6 (Kin.Dom.2-C-terminal) (K_d of 1,200 nM), Snark (K_d of 420 nM), Tnk1 (K_d of 640 nM) and Tyk2 (K_d of 620 nM). K562, KCL22, and THP-1 cells are exposed to different doses of STI571 or JAK inhibitors for 72 h to quantify the effects of tyrosine kinase inhibitor (TKI) activity. Cell growth inhibition is then evaluated using the MTT assay. The proliferation of K562 and KCL22 cells, but not THP-1 cells, is inhibited by IMA in a concentration-dependent manner. The IC₅₀ value of IMA is 0.28 µM for K562 and 0.17 µM for KCL22. Although treatment with Tofacitinib (TOF) or INCB018424 alone does not suppress cell proliferation, both Tofacitinib and INCB018424 make the K562 and KCL22 more sensitive to IMA.

In Vivo: Animals that are treated with Tofacitinib show a significantly lower production of anti-drug antibodies (ADAs) compare with PEG-treated control mice (for five weeks after initial immunization, p<0.01, n=8). Moreover ADAs become detectable earliest on day 28. A difference of 1000- to 200-fold in titers to SS1P is apparent from days 21 through 35, respectively. Compare to SS1P, mice injected with keyhole limpet hemocyanin (KLH) generate a more rapid antibody response. Yet, the administration of Tofacitinib reduces anti-KLH titers compare to controls (p<0.05 on day 21, p<0.01 on day 28, respectively, n=5). Reductions in titers ranged from 5000- to 250-fold from days 21 through 28, respectively. Based on previous dose-response studies, a daily dose of Tofacitinib of 6.2 mg/kg is selected to provide 80% inhibition of hind paw volume and plasma exposure capable of suppressing the JAK1 and JAK3 signaling pathways for >4 hours.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Apoptosis Compound Library  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Antiviral Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Antifungal Compound Library  |  Antibacterial Compound Library  |  NMPA-Approved Drug Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Obesity Compound Library  |  Anti-Liver Cancer Compound Library   |  Rare Diseases Drug Library  |  Children’s Drug Library  |  EMA-Approved Drug Library  |  FDA-Approved Anticancer Drug Library  |  Anti-Prostate Cancer Compound Library  |  Non-steroidal Anti-Inflammatory Compound Library  |  Cancer Stem Cells Compound Library  |  Pain-Related Compound Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  SY-5609  |  Antifungal agent 26  |  Myricetin 3-O-α-L-arabinopyranoside  |  BRD4 Inhibitor-18  |  Ganoderic acid TR  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  (1R,2S,7R)-Sitafloxacin-d₄ hydrochloride  |  Nebacumab  |  Gepotidacin  |  Amycolatopsin A  |  PC945  |  Antibiotic A-33853  |  Estradiol hemihydrate  |  AAPK-25  |  Sulbactam-d₂ sodium  |  Dutasteride-¹³C₆  |  Oleic acid-¹³C  |  Antimicrobial agent-5  |  NBTIs-IN-4  |  Proanthocyanidins  |  JAK-IN-20  |  Anticancer agent 120  |  Azlocillin sodium salt  |  Chitin synthase inhibitor 11  |  Abacavir sulfate  |  Antitubercular agent-13  |  Meloxicam-d₃-1  |  Thailanstatin D  |  SB-218078  |  Toyocamycin

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。