TG101209

• CAT Number: I005560
• CAS Number: 936091-14-4
• Molecular Formula: C26H35N7O2S
• Molecular Weight: 509.7
• 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: CC(C)(C)NS(C1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2C)=C1)(=O)=O

TG101209 (Cat.No:I005560) is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations; TG101209 inhibit BRD4 activity with IC50 of 130 nM. 

Reference

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 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 Article3: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 Article4: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 Article5: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