TG101209

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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.

Price and Availability

TG101209, purity > 98%, is in stock. The same day shipping after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406190Name: TG101209CAS#: 936091-14-4Chemical Formula: C26H35N7O2SExact Mass: 509.25729Molecular Weight: 509.67Elemental 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

Technical Data

Additional Information

References

1: Sun Y, Moretti L, Giacalone NJ, Schleicher S,Speirs CK, Carbone DP, Lu B. Inhibition of JAK2 signaling by TG101209enhances radiotherapy in lung cancer models. J Thorac Oncol. 2011Apr;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 JAK2inhibitor, has significant in vitro activity in multiple myeloma anddisplays 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 inhibitorTG101209 attenuates JAK2V617F levels and signaling and exertssynergistic cytotoxic effects against human myeloproliferativeneoplastic 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, FinkeC, Mak CC, Mesa R, Zhu H, Soll R, Gilliland DG, Tefferi A. TG101209, asmall molecule JAK2-selective kinase inhibitor potently inhibitsmyeloproliferative disorder-associated JAK2V617F and MPLW515L/Kmutations. Leukemia. 2007 Aug;21(8):1658-68. Epub 2007 May 31. PubMedPMID: 17541402.