|(2R,3S,4R,5S)-3-(3-氯-2-氟苯基)-4-(4-氯-2-氟苯基)-N-(4-((1-((S)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮杂-6-基)-2-氧代-6,9,12-三氧基-3-氮杂十四烷-14-基)氨甲酰基)-2-甲氧基苯基)-4-氰基-5-新戊基吡咯烷-2-酰胺|CsnPharm

CAS No.: 2064292-12-0

A1874 Catalog No. CSN23919

Synonyms: A1874

A1874 is a nutlin-based PROTAC targeting on BRD4, consist of a BRD4-ligand JQ1 linked to a MDM2 E3 ligase ligand RG7388.

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400-920-2911

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实验方案

技术信息

生物活性

描述A1874 is a nutlin-based PROTAC targeting on BRD4, consist of a BRD4-ligand JQ1 linked to a MDM2 E3 ligase ligand RG7388. A1874 possesses dual function as it dose-dependently degraded its target BRD4, accompanied with the downregulation of c-MYC, as well as stabilization of P53 and upregulated P21 due to the efficient engagement of MDM2 by RG7388 in HCT116 cells exposure to A1874 at concentration ranging in 100nM-10μM post 24h. A1874 at concentration of 100nM achieved a near-maximum degradation of BRD4 by 98%. Incubation with A1874 ultimately resulted in a 97% loss in HCT116 cell viability, much more potent than JQ1 or RG7388 alone, for a synergistic antiproliferative effect by the combination of the E3 ligase ligand and targeting warhead. It seems that the potency to cell viability of A1874 may corelate to the status of P53 as A1874 was less potent against the cell line with mutant P53 or P53 depletion. A1875 is the inactive version of A1874^[1].
参考文献

[1] Hines J, Lartigue S, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262.

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
- 0.8521 mL
- 4.2604 mL
- 8.5209 mL
- 5 mM
- 0.1704 mL
- 0.8521 mL
- 1.7042 mL
- 10 mM
- 0.0852 mL
- 0.4260 mL
- 0.8521 mL

技术信息

CAS号

2064292-12-0

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C58H62Cl3F2N9O7S

运输

蓝冰

分子量

1173.59

别名

A1874

溶解度

DMSO	100.0 mg/mL (85.2 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (85.2 mM)

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