ABBV-744

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Chemical Structure| 2138861-99-9 同义名 : -
CAS号 : 2138861-99-9
货号 : A464519
分子式 : C28H30FN3O4
纯度 : 99%+
分子量 : 491.55
MDL号 : MFCD31657409
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(213.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • BET
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 ... 展开 >> Acute Myeloid Leukemia (AML) 收起 << Phase 1 Recruiting April 13, 2020 United States, California ... 展开 >> 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 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.17mL

2.03mL

1.02mL

20.34mL

4.07mL

2.03mL
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.