生物活性

Obatoclax (GX15-070)是Bcl-2 homology domain-3 (BH3)的类似物，对各种抗凋亡的Bcl-2家族蛋白的IC50平均为3 uM，如对Mcl-1(IC50为2.9 uM)和Bfl-1(IC50为5 uM)。Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon. Obatoclax prevents the interaction of these pro-survival proteins with Bax or Bak, thereby inducing apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3. Obstoclax also induces autophagy in mouse embryo fibroblasts and in HeLa cells. This compound inhibits the growth of cancer cell lines and primary cancer isolates. Obatoclax enhances cytarabine-induced apoptosis by enhancing DNA DSBs. This novel mechanism provides compelling evidence for the clinical use of BH3 mimetics in combination with DNA-damaging agents in AML and possibly a broader range of malignancies.

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。