Bosutinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bosutinib 是一种 Bcr-Abl 激酶抑制剂，用于治疗费城染色体阳性 (Ph+) 慢性粒细胞白血病 (CML)。

Bosutinib is a Bcr-Abl kinase inhibitor for the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Compared to other tyrosine kinase inhibitors, it has a more favourable hematologic toxicity profile. FDA approved on September 4, 2012. (In Vitro):Bosutinib (SKI-606) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range.(In Vivo):Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (150 mg/kg; once daily, 5 days weekly) has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts.

Bosutinib (SKI-606) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range. Cell Proliferation Assay Cell Line:The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84)Concentration:0.1 μmol/L Incubation Time:72 h Result:Inhibited several human CML derived cell lines with IC50 values ranging from 1 to 20 nmol/L

Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (150 mg/kg; once daily, 5 days weekly) has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts. Animal Model:KU812CM L xenograft modelDosage:75 mg/kg twice daily or 150 mg/kg once daily Administration:Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) Result:Had the therapeutic activity and produced a dose- and schedule-dependent weight loss.Animal Model:Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts Dosage:150 mg/kg Administration:Bosutinib (150 mg/kg; once daily, 5 days weekly)Result:Decreased the rate of tumor growth and prolonged event-free survival of mice.

SKI 606

Tyrosine Kinase

Bcr-Abl

Abl| MAPK| c-Src

Cancer

——

380843-75-4

530.45

C26H29Cl2N5O3

>98% (HPLC)

Ethanol: 2 mg/mL (3.77 mM); DMSO: 100 mg/mL (188.51 mM)

N#CC1=C(NC2=CC(OC)=C(Cl)C=C2Cl)C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=C1

4-(2,4-dichloro-5-methoxyphenylamino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years