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CAS No.: 2138861-99-9

ABBV-744 Catalog No. CSN21197

Synonyms: ABBV-744

ABBV-744 is an inhibitor of BDII-selective BET bromodomain that is being investigated to treat AML and metastic castration-resistant prostate cancer.

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技术信息

生物活性

描述ABBV-744 is a selective BDII inhibitor with improved oral bioavailability. ABBV-744 exhibited antiproliferation to AML and androgen receptor (AR) positive prostate cancer cell line models, including models of Enzalutamide resistance. Consistent with this, ABBV-744 induced tumor growth inhibition in AML and prostate cancer xenograft models^[1]. Up to now, a phase1 study of ABBV-744 to acute myeloid leukaemia and prostate cancer is undergoing^[2].
作用机制ABBV-744 preferentially binds to BD2 of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones.^[3]
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03360006	Prostate Cancer ... more >> Acute Myeloid Leukemia (AML) Collapse <<	Phase 1	Recruiting	April 13, 2020	United States, California ... more >> UC Irvine /ID# 160789 Recruiting Orange, California, United States, 92868 UC Davis Comp Cancer Ctr /ID# 202729 Recruiting Sacramento, California, United States, 95817 United States, Illinois Northwestern /ID# 171098 Recruiting Chicago, Illinois, United States, 60611 University of Chicago /ID# 160702 Recruiting Chicago, Illinois, United States, 60637-1443 United States, Ohio Cleveland Clinic Foundation /ID# 160756 Recruiting Cleveland, Ohio, United States, 44195 United States, Texas Univ TX, MD Anderson /ID# 160701 Recruiting Houston, Texas, United States, 77030 United States, Washington Swedish-Center for Blood Disor /ID# 166487 Recruiting Seattle, Washington, United States, 98104 Collapse <<

参考文献

[1] Warren Kati. ABBV-744: A first-in-class highly BDII-selective BET bromodomain inhibitor. Cancer Research. Volume 78, Issue 13 Supplement, pp. DDT01-05.
[2] A Study Evaluating the Safety and Pharmacokinetics of ABBV-744 in Subjects With Advanced Prostate Cancer (CRPC) and Relapsed/Refractory Acute Myeloid Leukemia (AML) Cancer.
[3] BET inhibitor ABBV-744. NCI Drug Dictionary.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0344 mL
- 10.1718 mL
- 20.3436 mL
- 5 mM
- 0.4069 mL
- 2.0344 mL
- 4.0687 mL
- 10 mM
- 0.2034 mL
- 1.0172 mL
- 2.0344 mL

技术信息

CAS号

2138861-99-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H30FN3O4

运输

蓝冰

分子量

491.55

别名

ABBV-744

溶解度

DMSO	360.0 mg/mL (732.4 mM)
Water	insoluble

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