For research use only. Not for therapeutic Use.
TG101209（Cat No.:I005560）is a potent and selective inhibitor of Janus kinase 2 (JAK2), a key enzyme in the JAK-STAT signaling pathway involved in cytokine-mediated cellular processes such as proliferation, differentiation, and immune regulation. By inhibiting JAK2, TG101209 blocks abnormal signaling, making it valuable in cancer research, particularly for conditions like myeloproliferative disorders and leukemias associated with JAK2 mutations. Its specificity for JAK2 over other kinases also highlights its potential in targeted therapy development, providing insights into the role of JAK2 in disease progression and treatment strategies.
| Catalog Number | I005560 |
| CAS Number | 936091-14-4 |
| Synonyms | TG-101209 |
| Molecular Formula | C26H35N7O2S |
| Purity | ≥95% |
| Target | c-RET |
| Solubility | DMSO ≥100mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 6 nM (JAK2); 130 nM(BRD4) |
| IUPAC Name | N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide |
| InChI | InChI=1S/C26H35N7O2S/c1-19-18-27-25(29-20-9-11-22(12-10-20)33-15-13-32(5)14-16-33)30-24(19)28-21-7-6-8-23(17-21)36(34,35)31-26(2,3)4/h6-12,17-18,31H,13-16H2,1-5H3,(H2,27,28,29,30) |
| InChIKey | JVDOKQYTTYUYDV-UHFFFAOYSA-N |
| SMILES | CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)N4CCN(CC4)C |
| Reference | </br>1:The JAK2 blocker TG101209 is a potent inhibitor of clonogenic progenitor cell growth in patients with chronic myeloid leukaemia. Demyanets S, Jaeger E, Pablik E, Greiner G, Herndlhofer S, Valent P, Schwarzinger I.Br J Haematol. 2017 Feb 21. doi: 10.1111/bjh.14508. [Epub ahead of print] No abstract available. PMID: 28220937 </br>2:Inhibition of JAK2 signaling by TG101209 enhances radiotherapy in lung cancer models. Sun Y, Moretti L, Giacalone NJ, Schleicher S, Speirs CK, Carbone DP, Lu B.J Thorac Oncol. 2011 Apr;6(4):699-706. doi: 10.1097/JTO.0b013e31820d9d11. PMID: 21325979 Free PMC Article</br>3:TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells. Ramakrishnan V, Kimlinger T, Haug J, Timm M, Wellik L, Halling T, Pardanani A, Tefferi A, Rajkumar SV, Kumar S.Am J Hematol. 2010 Sep;85(9):675-86. doi: 10.1002/ajh.21785. PMID: 20652971 Free PMC Article</br>4:Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells. Wang Y, Fiskus W, Chong DG, Buckley KM, Natarajan K, Rao R, Joshi A, Balusu R, Koul S, Chen J, Savoie A, Ustun C, Jillella AP, Atadja P, Levine RL, Bhalla KN.Blood. 2009 Dec 3;114(24):5024-33. doi: 10.1182/blood-2009-05-222133. Epub 2009 Oct 14. PMID: 19828702 Free PMC Article</br>5:TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Pardanani A, Hood J, Lasho T, Levine RL, Martin MB, Noronha G, Finke C, Mak CC, Mesa R, Zhu H, Soll R, Gilliland DG, Tefferi A.Leukemia. 2007 Aug;21(8):1658-68. Epub 2007 May 31. PMID: 17541402 |
