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product name TG101209


References: Am J Hematol. 2010 Sep;85(9):675-86.



Molecular Weight (MW)

509.67
Formula

C26H35N7O2S
CAS No.

936091-14-4
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 102 mg/mL (200.12 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL (slightly soluble or insoluble)
Solubility (In vivo)

1% DMSO+30% polyethylene glycol+1% Tween 80: 12mg/mL
Chemical Name

N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19403323

TG101209 is an orally bioavailable, small molecule, ATP-competitive inhibitor towards several tyrosine kinases. TG101209 inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 of B200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 inducs cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3
In Vivo 100 mg/kg of TG101209 effectively prolongs the survival in JAK2V617F-induced disease (10 days). Compared with placebo-treated animals, TG101209-treated animals exhibit statistically significant, dose-dependent reduction in the circulating tumor cell burden at day +11 to 20%.
Animal model Ba/F3-V617F-GFP cells are injected into immunodeficient SCID mice to induce a rapidly fatal, fully penetrant hematopoietic disease.
Formulation & Dosage TG101209 is dissolved in DMSO; 100 mg/kg; oral gavage
References [1] Pardanani A, et al, Leukemia, 2007, 21(8), 1658-1668.

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