2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. 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。

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XY-06-007 Chemical Structure

XY-06-007 Chemical Structure

CAS No. : 2757045-94-4

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XY-06-007 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

XY-06-007 相关抗体:
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].

MCE 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
CAS 号
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

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

  • 方案 一

    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].

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

XY-06-007 相关分类

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XY-06-0072757045-94-4PROTACsEpigenetic Reader Domainbump-and-hole (B&H)PROTACBRD4BD1L94V degraderdegradationcereblonCRBNInhibitorinhibitorinhibit

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产品名称：
XY-06-007
目录号：
HY-145226
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