bs-7127C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 509.67

Formula: C26 H35 N7 O2 S

CAS Number: 936091-14-4

InChi Key: JVDOKQYTTYUYDV-UHFFFAOYSA-N

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)

Smiles: CN1CCN(CC1)C1C=CC(=CC=1)NC1N=C(NC2C=C(C=CC=2)S(=O)(=O)NC(C)(C)C)C(C)=CN=1

Purity: 98.0

Solubility: Soluble in DMSO, not in water

Appearance: Solid Power.

Shelf Life: 1.0 years

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.