XY-06-007

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

XY-06-007 

XY-06-007 是一种有效的选择性 B&H-PROTAC BRD4BD1L94V 降解剂。XY-06-007 对 BRD4BD1L94V 的 DC50, 6 h 为 10 nM。XY-06-007 且具有适合的体内药代动力学特征。

XY-06-007

XY-06-007 Chemical Structure

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生物活性

XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies[1].

IC50 & Target

Cereblon

 

体外研究
(In Vitro)

XY-06-007 shows a half-degradation concentration (DC50, 6 h) of 10.2±1.8 nM against BRD4BD1L94V with no degradation of off-targets, as assessed by whole proteome mass spectrometry[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

XY-06-007 has favorable pharmacokinetic profile, including good plasma concentration, area under the curve (AUC), and bioavailability. XY-06-007 exhibits short elimination half-life (0.515 h) due to relatively low clearance (21.9 mL/min/kg) following intravenous administration (2.0 mg/kg). XY-06-007 exhibits short elimination half-life (0.721 h) due to the Cmax (6.10 μM) and Tmax (0.25 h) following intraperitoneal injection (10 mg/kg)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six to eight weeks old male C57BL/6 mice[1]
Dosage: 2 mg/kg (iv) or 10 mg/kg (ip) (Pharmacokinetic Analysis)
Administration: Administered via tail vein injection or via intraperitoneal injection. Approximately 110 μL of blood/time point was collected into the K2EDTA tube via facial vein for bleeding for the time points: 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h.
Result: Maintained above its DC50, 6h of 10 nM for approximately 6 h when dosed at 10 mg/kg via intraperitoneal injection (IP), indicating that such in vivo degradation experiment would result in a favorable outcome.

分子量

809.27

Formula

C41H41ClN8O8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
  • 1.

    XY-06-007 is formulation: 0.4 mg/mL 5% DMSO + 5% solutol HS15 + 90% saline for vein injection (iv). XY-06-007 is formulation: 1.0 mg/mL 5% DMSO + 5% solutol HS15 + 90% saline for intraperitoneal injection (ip)[1].
参考文献

  • [1]. Radosław P Nowak, et al. Structure-Guided Design of a “Bump-and-Hole” Bromodomain-Based Degradation Tag. J Med Chem. 2021 Aug 12;64(15):11637-11650.

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