TG101209
TG101209, a small-molecule identified by structure based design, is a selective inhibitor of janus kinase 2 (Jak2) that potently inhibits Jak/Stat pathway in multiple myeloma (MM) cell lines, such as cell harboring JAK2V617F or MPLW515L/K mutations which are commonly associated with polycythemia vera (PV) and primary myelofibrosis (PMF) respectively. According to results of multiple studies, it has revealed that TG101209 exhibits a dose and time dependent cyctoxicity, which is associated with inhibited cell cycle progrgression and induced apoptosis, in a wild range of MM cell lines through suppressing the expression of pJak2, pStat3 and Bcl-xl and inducing the overexpression of pErk and pAkt.
Reference
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;85(9):675-686.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 509.67 |
| Cas No. | 936091-14-4 |
| Formula | C26H35N7O2S |
| Synonyms | TG-101209 |
| Solubility | ≥25.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)N4CCN(CC4)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | TG101209 is a selective inhibitor of JAK2 with IC50 of 6 nM. | |||||
| Targets | Flt3 | RET | JAK3 | |||
| IC50 | 6 nM | 25 nM | 17 nM | 169 nM | ||
Quality Control & MSDS
- View current batch:
Chemical structure
Related Biological Data
Related Biological Data
