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| Baricitinib (LY3009104, INCB028050)JAK1/JAK2 inhibitor,selective orally bioavailable |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.06%
- COA (Certificate Of Analysis)
- HPLC(Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
Related Biological Data
Related Biological Data
| Description | Baricitinib (LY3009104, INCB028050) is a selective inhibitor of JAK1 and JAK2with IC50 values of 5.9 nM and 5.7 nM, | |||||
| Targets | JAK2 | JAK1 | TYK2 | JAK3 | Chk2 | c-Met |
| IC50 | 5.7 nM | 5.9 nM | 53 nM | >400 nM | >1 μM | >10 μM |
| Kinase experiment [1]: | |
Inhibitory activities | Enzyme assays were performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or fulllength enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction was performed with or without Baricitinib (LY3009104, INCB028050) (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the Baricitinib (LY3009104, INCB028050) concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays were performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKa, IKKb, JNK1, Lck, MEK1, p38a, p70S6K, PKA, PKCa, Src, and ZAP70. |
| Cell experiment [1]: | |
Cell lines | Human PBMCs; PHA-stimulated T cells. |
Preparation method | Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 10, 100, 1000, 10000 nM; 48 h. |
Applications | In PBMCs, INCB028050 inhibits STAT3 phosphorylation stimulated by IL-6 and the production of chemokine MCP-1 with IC50 values of 44 and 40 nM, respectively. In isolated naive T-cells, INCB028050 inhibits STAT3 phosphorylation with IC50 value of 20 nM and inhibits the production of IL-17 and IL-22 with IC50 value of 50 nM. |
| Animal experiment [1]: | |
Animal models | Female rats; adjuvant-induced arthritis rats; DBA/1j arthritis mice induced by bovine type II collagen. |
Dosage form | Female rats: 10 mg/kg; 24 h; oral gavage.Adjuvant-induced arthritis rats: 1, 3, or 10 mg/kg; once daily for 2 wk; administrated orally.Collagen-induced arthritis (CIA) model: 1, 3, or 10 mg/kg; twice daily for 15 d; administrated orally. |
Preparation method | Suspended in 0.5% methylcellulose and given by oral gavage at 10 ml/kg. |
Applications | In female rats, INCB028050 (10 mg/kg) inhibits JAK1/2 signaling by ≥50% for 8 h. In rat adjuvant-induced arthritis, INCB028050 (1, 3, or 10 mg/kg) reduces disease scores by 24%, 57% and 81% respectively and inhibits the increase of hind paw volumes by 50%, >95% and >95%, respectively. Also, INCB028050 reduced bone resorption. In CIA mice model, INCB028050 (1, 3, or 10 mg/kg) reduces clinical scores by 19%, 67% and 61% respectively and inhibits IL-6 and IL-23 signaling and function. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Fridman JS, Scherle PA, Collins R, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol, 2010, 184(9): 5298-5307. | |
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| Cas No. | 1187594-09-7 | SDF | Download SDF |
| Synonyms | INCB 028050,INCB-028050,LY 3009104,LY-3009104 | ||
| Chemical Name | 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile | ||
| Canonical SMILES | CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 | ||
| Formula | C16H17N7O2S | M.Wt | 371.42 |
| Solubility | ≥18.57 mg/mL in DMSO, <2.46 mg/ml="" in="" etoh,=""><2.58 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Baricitinib, formerly named LY3009104 or INCB028050, is a new selective orally bioavailable inhibitor of tyrosine-protein kinase JAK1 or JAK2. Also, it is an ATP competitive kinase inhibitor. In vitro, it is able to inhibit JAK1 and JAK2 in a low nanomolar range with IC50 values of 5.9 and 5.7 nM, respectively, while it demonstrates low inhibitory activity for JAK3 and moderate activity for TYK2. Baricitinib inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. It should also be recognized that JAK signaling is central to a number of fundamental processes, including the generation of RBCs
Reference
Gras, J. Baricitinib. Tyrosine-protein kinase JAK1/JAK2 inhibitor, treatment of rheumatoid arthritis. Drugs of the future. 2013, 38(9): 611.
Jordan S. Fridman, Peggy A. Scherle, Robert Collins, Timothy C. Burn, Yanlong Li, Jun Li, Maryanne B. Covington, Beth Thomas, Paul Collier, Margaret F. Favata, Xiaoming Wen, Jack Shi, Ryan McGee, Patrick J. Haley, Stacey Shepard, James D. Rodgers, Swamy Yeleswaram, Greg Hollis, Robert C. Newton, Brian Metcalf, Steven M. Friedman and Kris Vaddi. Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050. The Journal of Immunology May 1, 2010 vol. 184 no. 9 5298-5307.
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配后是否应该分装,因为不能反复冻融?
多谢!
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【】可以这样输入，智能ABC，输入“v1”，后翻3页，就可以看见了，或用紫光拼音中文输入法，输入方括号就是粗体的中括号，实在不行请复制本公告中【】
同一管dna有的酶可以切开，比如dra1，ecoR1,Hind111
有的酶又完全不能切动，如BamH1，sac1，xba1，xho1，pst1
请问高手这是什么原因？?
感谢赐教~！
求问酶切体系为10ul,内切酶1ul,37℃水浴45min，不知道DNA产物是否完全被切开了？
所用内切酶信息如下
我做的双酶切反应，酶分别是宝生物的BamHI和XhoI，双酶切体系是：载体及目的片段分别是30ul，通用buffer4ul，XhoI、BamHI各2ul，无核酶水2ul，总体积40ul。载体和目的片段都是经37度酶切6h。载体上面这两个酶切位点的距离是6个碱基，目的片段是由pcr反应获得的，从puc19中p出来的，两端带有这两种酶的酶切位点，酶切完成后，做连接反应，体系如下：目的片段（全长1441bp）4ul，无核酶水3ul，10*T4DNA连接酶缓冲液1ul，载体1ul，T4DNA连接酶1ul，总体积10ul。16度过夜。之后摇菌送沉菌测序结果回来，送了5管一个都不对。重复实验两次还是不对！
之后改为先用BanHI单切载体，体系如下：载体17ul，酶1ul，buffer2ul，总体积20ul，30度切6小时后，Promega纯化试剂盒直接纯化，完了之后再用XhoI，37度酶切6小时，体系如上，再次用promega纯化试剂盒纯化，目的片段用双酶切体系酶切，之后做连接反应，之后铺板，挑取菌落共10个，摇菌13小时，取菌液做pcr鉴定，结果10个菌落全是引物2聚体，跑出来的条带都是100bp左右。
各位老师这是怎么回事呢？为什么连接不上呢？小弟先谢过各位大哥了！
