2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. XY-06-007

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.

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XY-06-007

XY-06-007 構造式

CAS 番号 : 2757045-94-4

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1 mg $490 在庫あり
5 mg $1225 在庫あり
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XY-06-007 関連抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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製品説明

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

 

体外実験

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].

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

XY-06-007 関連抗体
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 Cmax (6.10 μM) and Tmax (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.
分子量

809.27

分子式

C41H41ClN8O8
CAS 番号
Appearance

Solid

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

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

一般には略語で表示されます：C1V1 = C2V2

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C1

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体積 （開始）

V1

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体積 （終了）

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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].

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参考文献
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XY-06-007 Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品名:
XY-06-007
製品番号:
HY-145226
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