2023年3月1日 · XL102 is a potent, orally bioavailable, highly selective covalent CDK7 inhibitor. QUARTZ-101 is a first-in-human, open-label trial (NCT04726332) evaluating the safety, tolerability, and optimal dose of XL102 as a single agent and in combination regimens in patients with solid tumors, with expansion in subsequent tumor cohorts of advanced HR+ BC ...

In the dose-escalation stage (modified interval 3+3 design), a maximum tolerated dose and/or recommended dose (MTD/RD) of XL102 will be established (primary endpoint) for use alone (solid tumors) and then for use in combination with standard dose fulvestrant (HR+BC) or abiraterone/prednisone (mCRPC); dose escalation will require ̃36 pts for ...

2023年7月29日 · The data suggests XL102 induces apoptosis in AML cells via CDK7/c-Myc/p53 axis. RNA-sequencing from paired Venetoclax-sensitive and Venetoclax-resistant cells treated with XL102 showed downregulation of genes involved in proliferation and apoptosis.

2022年2月15日 · XL102 induced cell death in a number of cancer cell lines and caused tumor regression in murine xenograft models of multiple tumor types including HR+ BC and TNBC. Here, we present the study design of an ongoing phase 1 trial in solid tumors which includes cohorts with advanced HR+ BC, TNBC, epithelial ovarian cancer (EOC), and metastatic ...

2023年7月29日 · • XL102 is a novel, highly specific, orally bioavailable covalent inhibitor of CDK7 • CDK7 inhibition induces cell cycle arrest and apoptosis via CDK7/c-Myc/p53 axis in AML • XL102 synergizes with Venetoclax in AML

xl102，一种高度特异性、口服生物利用度的 cdk7 共价抑制剂。xl102 在原发性骨髓细胞 (n = 54) 中对 cdk7 的抑制作用在纳摩尔范围内（平均值 = 300 nm；范围 = 4.0-952 nm）。xl102 处理的 aml 细胞显示 rna 聚合酶 ii 羧基末端结构域丝氨酸 2/5/7 磷酸化水平降低。

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tps3176 背景： xl102 是一种可口服的、选择性的、共价的细胞周期蛋白依赖性激酶 7 (cdk7) 小分子抑制剂。cdk7 是一种在多种肿瘤类型中过度表达的丝氨酸/苏氨酸激酶。cdk7 通过 cdk（1、2、4 和 6）的磷酸化控制细胞周期进程，并通过 rna 聚合酶 ii 的磷酸化调节转录。

Background: XL102 is an orally bioavailable, selective, and covalent small-molecule inhibitor of cyclin-dependent kinase 7 (CDK7). CDK7 is a serine/threonine kinase that is overexpressed in multiple tumor types. CDK7 controls cell cycle progression via the phosphorylation of CDKs (1, 2, 4, and 6) and regu-

An orally bioavailable, selective inhibitor of cyclin-dependent kinase 7 (CDK7), with potential antineoplastic activity. Upon oral administration, CDK7 inhibitor XL102 selectively targets, covalently binds to and inhibits the activity of CDK7, thereby inhibiting CDK7-mediated signaling.