XY-06-007

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XY-06-007

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2757045-94-4

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

XY-06-007 是一种有效的选择性 B&H-PROTAC BRD4_BD1L94V降解剂。XY-06-007 对BRD4_BD1L94V的DC_{50, 6 h}为 10 nM。XY-06-007 且具有适合的体内药代动力学特征。

生物活性

XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTACBRD4_BD1L94V degrader. XY-06-007 shows aDC_{50, 6 h}of 10 nM againstBRD4_BD1L94V 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 BRD4_BD1L94V with no degradation of off-targets, as assessed by whole proteome mass spectrometry^[1].

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 C_max(6.10 μM) and T_max(0.25 h) following intraperitoneal injection (10 mg/kg)^[1].

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

CAS 号

2757045-94-4

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].