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製品番号: HY-145226

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XY-06-007

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Based on 1 Customer Validation

XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4_BD1L94V degrader. XY-06-007 shows a DC_{50, 6 h} of 10 nM against BRD4_BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies.
(Pink: BRD4 BD1L94V ligand (HY-184949); Blue: Cereblon ligand (HY-103597); Black: linker).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 98.9%
CAS 番号: 2757045-94-4
分子式: C₄₁H₄₁ClN₈O₈
分子量:809.27

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

XY-06-007 構造式

CAS 番号: 2757045-94-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体内
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4_BD1L94V degrader. XY-06-007 shows a DC_{50, 6 h} of 10 nM against BRD4_BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies^[1]. (Pink: BRD4 BD1L94V ligand (HY-184949); Blue: Cereblon ligand (HY-103597); Black: linker).

IC₅₀ & Target

Cereblon

PROTACs アイソフォーム固有の製品をすべて表示 :

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

体外実験

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].

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

体内実験

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].

MedChemExpress (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.

化学情報

CAS 番号 2757045-94-4
性状 Solid
分子量 809.27
分子式 C₄₁H₄₁ClN₈O₈
Color White to off-white
SMILES

ClC1=CC=C(C2=N[C@H](C3=NN=C(N3C4=C2C=C(C=C4)OC)C)[C@H](C(NCCCCCNC(COC5=C6C(C(N(C6=O)C7C(NC(CC7)=O)=O)=O)=CC=C5)=O)=O)C)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

View the Complete Stock Solution Preparation Table

体内:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 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].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (273 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

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. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体内実験
純度とドキュメンテーション
参考文献

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XY-06-007

PROTACs アイソフォーム固有の製品をすべて表示

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示