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TL02-59
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TL02-59图片
CAS NO:1315330-17-6
包装与价格:
包装价格(元)
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产品介绍
TL02-59 是一种口服活性,选择性的 Src-家族激酶 Fgr 抑制剂,IC50 为 0.03 nM。TL02-59 也抑制 Src-家族激酶 Lyn 和 Hck,IC50 分别为 0.1 nM 和 160 nM。TL02-59 有效抑制急性髓性白血病 (AML) 细胞生长。
Cas No.1315330-17-6
Canonical SMILESO=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(OC4=C5C=C(OC)C(OC)=CC5=NC=N4)=C3
分子式C32H34F3N5O4
分子量609.64
溶解度DMSO: 125 mg/mL (205.04 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 also inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth[1].

TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency[1]. TL02-59 induces growth arrest in primary AML bone marrow samples[1]. TL02-59 (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation in TF-1 cells, with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range[1]. Western Blot Analysis[1] Cell Line: TF-1 myeloid cells

TL02-59 (oral administration; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement[1]. TL02-59 has a t1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively[1]. Animal Model: NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells

[1]. Weir MC, et al. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 Jun 15;13(6):1551-1559.