ARQ 621 是一种变构和选择性 Eg5 有丝分裂运动蛋白抑制剂,具有抗肿瘤活性。
产品描述
ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.
体外活性
ARQ 621 demonstrates anti-tumor activity against a wide range of human cancer cell lines in vitro, including colon, lung, endometrial, bladder, and hematologic cancer cell lines, with significantly less cytotoxicity against hematopoietic cells. [1]
体内活性
ARQ 621, as a novel clinical stage drug candidate, inhibits a number of xenografts grown in athymic mice, such as pancreatic, breast, prostate, and ovarian carcinomas with no hematological changes. Furthermore, for ARQ 621, there is no envidence of bone marrow toxicity in pre-clinical mouse efficacy models or safety studies in rats and dogs. [1]
Cas No.
1095253-39-6
分子式
C28H24Cl2FN5O2
分子量
552.43
储存和溶解度
H2O:<1 mgml
Ethanol:93 mg/mL (168.3 mM)
DMSO:93 mg/mL (168.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years