产品
编 号：F288815
分子式：C32H36Cl2F3N5O4
分子量：682.56
分子式：C32H36Cl2F3N5O4
分子量：682.56
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CAS No: 2415263-06-6
产品详情
生物活性：
TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.
体内研究：
TL02-59 (oral; 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. TL02-59 has a t1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively.Animal Model:NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells
Dosage:1 and 10 mg/kg
Administration:Oral; for three weeks
Result:Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.
体外研究：
TL02-59 dihydrochloride (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. TL02-59 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples.
TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.
体内研究：
TL02-59 (oral; 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. TL02-59 has a t1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively.Animal Model:NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells
Dosage:1 and 10 mg/kg
Administration:Oral; for three weeks
Result:Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.
体外研究：
TL02-59 dihydrochloride (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. TL02-59 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples.
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