TG101209 Inhibitor CAS No. 936091-14-4

Cat. No.	Name	Size	Price
KI1173	TG101209	5 mg	$272
	TG101209	10 mg	$512
	TG101209	50 mg	$1552
	TG101209	200 mg	$3952

Chemical Characteristic

Product Name	TG101209
CAS No.	936091-14-4
Molecular Weight	509.67
Formula	C₂₆H₃₅N₇O₂S
Chemical Name	N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
Smiles	c1(cc(ccc1)Nc1nc(ncc1C)Nc1ccc(cc1)N1CCN(CC1)C)S(=O)(=O)NC(C)(C)C
Chemical Structure

Biological activities

TG101209 potently inhibits JAK2, FLT3 and RET kinases with IC50 values of 6, 25 and 17 nM, respectively. TG101209 shows significantly less activity against JAK3 tyrosine kinases with IC50 value of 169 nM. In vitro, TG101209 inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of about 200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 (1.2 µM) induces cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3.^[1] Furthermore, TG101209 (2 µM) attenuates JAK2V617F autophosphorylation and induces apoptosis of HEL92.1.7 and Ba/F3-JAK2V617F cells in vitro.^[2] In vivo, TG101209 (100 mg/kg) is effective in a mouse model of JAK2V617F-induced hematopoietic disease.^[1] In HCC2429 lung cancer xenograft model, combination of TG101209 (100 mg/kg) and radiation significantly prolongs tumor growth delay. TG101209 (100 mg/kg) also reduces tumor proliferation and vascular density, and increases apoptosis in the irradiated lung cancer mouse xenografts.^[3]

Protocols

In vitro: TG101209 is dissolved in DMSO.^[1]

References

[1] Pardanani A, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007, 21(8): 1658-1668. [2] Wang Y, et al. Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells. Blood. 2009, 114(24): 5024-5033. [3] Sun Y, et al. Inhibition of JAK2 signaling by TG101209 enhances radiotherapy in lung cancer models. J Thorac Oncol. 2011, 6(4): 699-706.

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