WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406190
CAS#: 936091-14-4
Description: TG101209 is a novel and potent JAK2 inhibitor, which induced dose- and time-dependent cytotoxicity in a variety of multiple myeloma (MM) cell lines. The induction of cytotoxicity was associated with inhibition of cell cycle progression and induction of apoptosis in myeloma cell lines and patient-derived plasma cells. Exploring the mechanism of action of TG101209 indicated downregulation of pJak2, pStat3, and Bcl-xl levels with upregulation of pErk and pAkt levels indicating cross talk between signaling pathways. TG101209 , when used in combination with the PI3K inhibitor LY294002, demonstrated synergistic cytotoxicity against myeloma cells.
MedKoo Cat#: 406190
Name: TG101209
CAS#: 936091-14-4
Chemical Formula: C26H35N7O2S
Exact Mass: 509.25729
Molecular Weight: 509.67
Elemental Analysis: C, 61.27; H, 6.92; N, 19.24; O, 6.28; S, 6.29
Synonym: TG101209; TG-101209; TG 101209
IUPAC/Chemical Name: N-tert-butyl-3-(5-methyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide
InChi Key: JVDOKQYTTYUYDV-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=S(C1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O
1: Sun Y, Moretti L, Giacalone NJ, Schleicher S, Speirs CK, Carbone DP, Lu B. Inhibition of JAK2 signaling by TG101209 enhances radiotherapy in lung cancer models. J Thorac Oncol. 2011 Apr;6(4):699-706. doi: 10.1097/JTO.0b013e31820d9d11. PubMed PMID: 21325979; PubMed Central PMCID: PMC3104103.
2: Ramakrishnan V, Kimlinger T, Haug J, Timm M, Wellik L, Halling T, Pardanani A, Tefferi A, Rajkumar SV, Kumar S. TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells. Am J Hematol. 2010 Sep;85(9):675-86. doi: 10.1002/ajh.21785. PubMed PMID: 20652971; PubMed Central PMCID: PMC2940994.
3: 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. Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells. Blood. 2009 Dec 3;114(24):5024-33. doi: 10.1182/blood-2009-05-222133. Epub 2009 Oct 14. PubMed PMID: 19828702; PubMed Central PMCID: PMC2788976.
4: 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. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007 Aug;21(8):1658-68. Epub 2007 May 31. PubMed PMID: 17541402.
