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TG101209
Synonyms:
CAS NO: 936091-14-4
Molecular Formula: C26H35N7O2S
Molecular Weight: 509.67
Purity: 98% min
Solubility: In DMSO
Storage: −20°C
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Remarks: TG101209 is a potent and small molecule JAK2-selective kinase inhibitor with IC50 of 6, 25, 17 and 169 nM for JAK2, FLT3, RET and JAK3, respectively.TG101209 potently prevents myeloproliferative disorder-related JAK2V617F and MPLW515L/K mutations. Besides, TG101209 suppressed the activation of STAT3 and survivin expression and sensitized HCC2429 and H460 cells to radiation in clonogenic assays. After treatment with TG101209, phospho-ERK protein levels were decreased in both HCC2429 and H460 cells. HCC2429 cells transfected with KRAS-12V mutant were more resistant to radiation- and TG101209-evoked apoptosis than wild-type control cells. In vivo, addition of TG101209 to radiation in lung xenografts produced a striking tumor growth delay (>10 days) compared with radiation alone and was well tolerated. Immunohistochemistry staining of tumor sections showed that TG101209 enhanced apoptosis and decreased cell proliferation and vascular density, suggesting that TG101209 also has antiangiogenic effects.

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