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 Chemical Structure

XY-06-007 Chemical Structure

CAS No. : 2757045-94-4

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XY-06-007 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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

 

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].

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

XY-06-007 Related Antibodies
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].

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.
Molecular Weight

809.27

Formula

C41H41ClN8O8
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility

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In Vivo:

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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Purity & Documentation
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XY-06-007 Related Classifications

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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