|(S)-2-(6-(4-氯苯基)-8-甲氧基-1-甲基-4H-苯并[f][1,2,4]三唑[4,3-a][1,4]二氮杂卓-4-基)-N-乙基乙酰胺|CsnPharm

CAS No.: 1260907-17-2

Molibresib Catalog No. CSN13061

Synonyms: I-BET762;GSK525762;GSK525762A

I-BET 762 is an inhibitor for BET proteins with IC50 of ~35 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bromodomain BET

IC50:~35nM
描述The Bromodomain and Extra-Terminal Domain BET (Bromodomain and Extra-Terminal Domain) family is characterized by the presence of two tandem bromodomains and an extra-terminal domain. BET proteins can govern the assembly of histone acetylation-dependent chromatin complexes, thus regulating gene expression. I-BET-762 is a highly selective BET protein inhibitor with IC50 values of 32.5–42.5nM (measured by FRET analysis). I-BET-762 can suppress the inflammatory gene expression, including LPS-inducible Il6, Ifnb1, Il1b, Il12a, Cxcl9, Ccl12 and IL-1b processing enzyme Mefv, as well as diminish expression of transcription factors Rel, Irf4 and Irf8 in BMDMs. In contrast, I-BET762 only has a marginal effect on general gene transcription in macrophages without LPS-stimulation. Injection of I-BET-762, 30mg/kg, i.v., 1h before or 1.5 h after LPS administration can attenuate death of mice. Twice-daily injections of I-BET-762, 30mg/kg, i.v., for 2 days protected mice against death caused by sepsis^[1]. A phase 1 study of I-BET762 in combination with androgen deprivation therapy treatment for castrate-resistant prostate cancer and a phase 2 study of I-BET762 in combination with Fulvestrant treatment for ER+ breast cancer is recruiting (see https://clinicaltrials.gov/).
作用机制I-BET-762 can interact with the BRD pocket in the manner of competition with acetylated peptide binding and displace BET proteins from acetylated chromatin in cells.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
Rosetta2 DE3 cells	-	Function assay	30 mins	Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=30.3 nM	26080064

动物研究

剂量

Mice: 8 mg/kg - 25 mg/kg^[3] (p.o.), 10 mg/kg^[4] (i.p.)

给药途径

p.o., i.p.

动物药代数据

Animal	Mice^[5]
Dose	1 mg/kg
Administration	i.v.
PAMPA	High
T_1/2	1.22 h
CL	12.57 ml/min/kg
AUC_0→last	1299 ng·h/ml
Vd_ss	1.11 L/kg

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
NCT03702036	-	-	-	-	-
NCT02706535	Drug Interactions	Phase 1	Completed	-	United States, Maryland ... more >> GSK Investigational Site Baltimore, Maryland, United States, 21225 Collapse <<
NCT03266159	Solid Tumours	Phase 2	Withdrawn(Study withdrawn befo... more >>re active to fully evaluate impact of changing practice in target population.) Collapse <<	August 19, 2020	-

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
- 2.3591 mL
- 11.7954 mL
- 23.5907 mL
- 5 mM
- 0.4718 mL
- 2.3591 mL
- 4.7181 mL
- 10 mM
- 0.2359 mL
- 1.1795 mL
- 2.3591 mL

技术信息

CAS号

1260907-17-2

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

C22H22ClN5O2

运输

蓝冰

分子量

423.90

别名

I-BET762;GSK525762;GSK525762A;molibresib

溶解度

DMSO	650.0 mg/mL (1533.4 mM) warming
Water	1.0 mg/mL (2.4 mM) warming

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	13 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03702036	-	-	-	-	-
NCT02706535	Drug Interactions	Phase 1	Completed	-	United States, Maryland ... more >> GSK Investigational Site Baltimore, Maryland, United States, 21225 Collapse <<
NCT03266159	Solid Tumours	Phase 2	Withdrawn(Study withdrawn befo... more >>re active to fully evaluate impact of changing practice in target population.) Collapse <<	August 19, 2020	-
NCT03150056	Solid Tumours	Phase 1	Recruiting	July 29, 2019	-
NCT02964507	Neoplasms	Phase 2	Recruiting	June 1, 2020	-
NCT01587703	Carcinoma, Midline	Phase 1	Active, not recruiting	December 14, 2018	United States, Maryland ... more >> GSK Investigational Site Baltimore, Maryland, United States, 21231-2410 United States, Massachusetts GSK Investigational Site Boston, Massachusetts, United States, 02215 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19104 United States, Tennessee GSK Investigational Site Nashville, Tennessee, United States, 37232 United States, Texas GSK Investigational Site Houston, Texas, United States, 77030 Australia, Victoria GSK Investigational Site Clayton, Victoria, Australia, 3168 Canada, Alberta GSK Investigational Site Edmonton, Alberta, Canada, T6G 1Z2 France GSK Investigational Site Bordeaux Cedex, France, 33076 GSK Investigational Site Lyon Cedex 08, France, 69373 GSK Investigational Site Paris Cedex 5, France, 75248 Korea, Republic of GSK Investigational Site Seoul, Korea, Republic of, 03080 GSK Investigational Site Seoul, Korea, Republic of, 03722 Netherlands GSK Investigational Site Amsterdam, Netherlands, 1066 CX Spain GSK Investigational Site Barcelona, Spain, 08035 GSK Investigational Site Madrid, Spain, 28040 GSK Investigational Site Málaga, Spain, 29010 United Kingdom GSK Investigational Site Sutton, Surrey, United Kingdom, SM2 5PT GSK Investigational Site Newcastle upon Tyne, United Kingdom, NE7 7DN Collapse <<
NCT01943851	Cancer	Phase 1	Recruiting	September 26, 2022	United States, Arkansas ... more >> GSK Investigational Site Recruiting Little Rock, Arkansas, United States, 72205 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Colorado GSK Investigational Site Recruiting Aurora, Colorado, United States, 80045 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, New York GSK Investigational Site Recruiting New York, New York, United States, 10065 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Pennsylvania GSK Investigational Site Completed Philadelphia, Pennsylvania, United States, 19104 United States, Texas GSK Investigational Site Recruiting Houston, Texas, United States, 77030 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Australia, Victoria GSK Investigational Site Recruiting East Melbourne, Victoria, Australia, 3002 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Korea, Republic of GSK Investigational Site Not yet recruiting Seoul, Korea, Republic of, 03722 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Seoul, Korea, Republic of, 06351 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Spain GSK Investigational Site Recruiting Barcelona, Spain, 08036 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Madrid, Spain, 28006 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Madrid, Spain, 28040 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Málaga, Spain, 29010 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Salamanca, Spain, 37007 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United Kingdom GSK Investigational Site Recruiting Cambridge, United Kingdom, CB2 0QQ Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Completed London, United Kingdom, W12 0NN Collapse <<

Molibresib Catalog No. CSN13061

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