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TL02-59

CAS No. : 1315330-17-6

MCE 站：TL02-59

产品活性：TL02-59 是一种具有口服活性，选择性的 Src-家族激酶 Fgr 抑制剂，IC₅₀ 为 0.03 nM。TL02-59 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。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：Src  |  Apoptosis

In Vitro: 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.
TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency.
TL02-59 induces growth arrest in primary AML bone marrow samples.

In Vivo: 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.
TL02-59 has a t_1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively.

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Reprogramming Compound Library  |  Orally Active Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Acetylcysteine  |  Angiotensin II human  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Verteporfin  |  Decitabine  |  Actinomycin D  |  Temozolomide  |  BAY 11-7082  |  Etoposide  |  Mitomycin C  |  CCCP  |  DAPT  |  Rotenone  |  Etomoxir  |  Stattic  |  Docetaxel  |  Fulvestrant

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