2019年7月1日 · Here, we describe a selective CDK7 inhibitor SY-1365, which is currently in clinical trials in populations of patients with ovarian and breast cancer (NCT03134638). In …

SY-1365, a CDK7 inhibitor has shown initial encouraging data in phase I for solid tumors treatment. These results have rejuvenated the CDKs research field. This review provides an …

Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a K i of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib …

2017年7月1日 · SY-1365 was screened in a panel of solid tumor cell lines, revealing activity in breast, ovarian, colorectal and lung cancer cells with low nM EC 50 and rapid induction of …

2017年12月8日 · SY-1365, a selective inhibitor of CDK7, was developed to exploit tumor dependencies driven by CDK7 and is in clinical development in patients with advanced solid …

New data on SY-1365, a first-in-class selective CDK7 inhibitor currently in a Phase 1 clinical trial, suggest that RB pathway alterations are predictive of response in preclinical models of high …

2020年12月10日 · sy-1365通过下调致癌转录因子、抗凋亡蛋白(例如，mcl1和myc)、调控细胞周期与dna修复(尤其是，同源重组修复和错配修复)进展的通路来介导其抗癌活性，从而导 …

SY-1365处理可降低MCL1蛋白水平，并且发现低BCL2L1（BCL-XL）表达的癌细胞对SY-1365更敏感。 急性髓细胞性白血病（AML）细胞系的转录变化与其他转录抑制剂处理后的变化不同 …

Preclinical studies in solid tumor and hematologic malignancies show treatment with SY-1365 leads to antitumor activity, showing apoptosis in vitro and complete regressions in xenograft …

SY-1365 Shows Synergistic Anti-Tumor Activity in Combination with Carboplatin in Preclinical Models of Ovarian Cancer, Supporting Ongoing Investigation of the Combination in Phase 1 …