dBET6

Dangerous Goods

CAS number：1950634-92-0 molecular formula：C42H45ClN8O7S

overview

Specs

numbering system

physicochemical properties

Safety information

Production methods and uses

MSDS

overview

compound introduction

Information dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis . Targets BRD4 14 nM In vitro dBET6 is a highly cell-permeable degrader of BET bromodomains. It is potent in most cancer cell lines. dBET6 features highly increased cellular potency with evident degradation in the sub-nanomolar range. Treatment with 100 nM dBET6 leads to degradation of BRD4 after 1 hr, prompting subsequent downregulation of c-MYC and induction of apoptosis. dBET6 disrupts global productive transcription elongation. dBET6 treatment leads to a widespread decrease in steady-state mRNA levels, but observed an incommensurate impact on expression of members of the core regulatory circuitry of leukemogenic transcription factors. The collapse of the core transcriptional machinery prompted by BET degradation precedes a robust apoptotic response, of apparent translational significance. In vivo dBET6 is well tolerated. Upon dBET6 treatment, a significant reduction of leukemic burden is observed in a disseminated mouse model of T-ALL. Moreover, mice treated with dBET6 (7.5 mg/kg BID) exhibits a significant survival benefit compared to mice treated with vehicle control or JQ1 (20 mg/kg QD). Cell Research(from reference) Cell lines：MOLT4 cells deficient in CRBN expression Concentrations：0.05, 0.1, 0.5, 1 μM Incubation Time：3 hr

Specs

Chinese alias	-
English alias	dBET6 \| 1950634-92-0 \| 2-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(8-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)octyl)-acetamide \| 2-((S)-4-(4-chlorophenyl)-2,3,9-trim
CAS number	1950634-92-0	molecular formula	C42H45ClN8O7S
molecular weight	841.37 g/mol	Exact mass	-
PSA	222.000 Å²	logp	4.8

numbering system

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Safety information

pictogram：

GHS06 , GHS08

Signal word：

Danger

Hazard Statement：

H301: 吞咽会中毒 H360: 可能损害生育力或未出生的孩子

Statement of Preventive Measures：

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P203: 使用前，获取、阅读并遵守所有安全说明。 P301+P316: 如果吞咽：立即寻求紧急医疗救助。 P318: 如果暴露或担心，请就医。