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Referencia número: HY-145226

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XY-06-007

Name: XY-06-007
Brand: MedChemExpress
SKU: HY-145226
Price: 490.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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XY-06-007 is a mutation-selective PROTAC degrader targeting BRD4_BD1L94V, with a DC_{50, 6 h} of 10.2 nM in Flp293T cells. XY-06-007 recruits the E3 ligase CRL4CRBN to BRD4_BD1L94V, triggering ubiquitination and proteasomal degradation. XY-06-007 can be combined with the dTAG strategy to achieve degrader-mediated synchronous depletion of the corresponding protein fusion in cells. XY-06-007 is applicable for cancer research.
(Pink: BRD4 BD1L94V ligand (HY-184949); Blue: Cereblon ligand (HY-103597); Black: linker).

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 98.9%
No. CAS: 2757045-94-4
Fòrmula: C₄₁H₄₁ClN₈O₈
Peso molecular:809.27

Almacenamiento:

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

XY-06-007 Chemical Structure

No. CAS: 2757045-94-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Solvente y solubilidad
- In Vivo
Protocolo (1)
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

XY-06-007 is a mutation-selective PROTAC degrader targeting BRD4_BD1L94V, with a DC_{50, 6 h} of 10.2 nM in Flp293T cells. XY-06-007 recruits the E3 ligase CRL4CRBN to BRD4_BD1L94V, triggering ubiquitination and proteasomal degradation. XY-06-007 can be combined with the dTAG strategy to achieve degrader-mediated synchronous depletion of the corresponding protein fusion in cells. XY-06-007 is applicable for cancer research^[1]. (Pink: BRD4 BD1L94V ligand (HY-184949); Blue: Cereblon ligand (HY-103597); Black: linker).

IC₅₀ & Target

^[1]

BRD4BD1L94V

Cereblon

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas Epigenetic Reader Domain :

Cellular Effect

Cell Line	Type	Value	Description	References
Flp-In-293	DC₅₀	10.2 nM	Half-maximal degradation of BRD4 BD1 L94V-EGFP in Flp293T cells incubated for 5 h, measured via EGFP:mCherry ratio using an Acumen High Content Imager. Half-maximal degradation of BRD4 BD1 L94V-EGFP in Flp293T cells incubated for 5 h, measured via EGFP:mCherry ratio using an Acumen High Content Imager.	34279939

In Vitro

XY-06-007 potently binds to the mutant bromodomains BRD4 BD1^L94V, BRD4 BD2^L387V, and BRD2 BD2^L383V, with corresponding IC₅₀ values of 132 nM, 438 nM, and 145 nM, respectively; in contrast, its binding affinity to wild-type BRD4 BD1 and BRD4 BD2 is significantly weaker, with corresponding IC₅₀ values of 1260 nM and 3505 nM^[1].
XY-06-007 (5 h) potently and selectively degrades BRD4 BD1 L94V-EGFP in Flp293T cells, with a DC₅₀,₆ₕ of 10.2 nM^[1].
XY-06-007 (5-7 h) selectively degrades BRD4 BD1 L94V-EGFP without cross-degrading FKBP12 fusion proteins in Flp293T cells co-expressing HiBit-FKBP12 F36V-KRAS^G12C^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Parmacokinetics

Species	Dose	Route	T_max	C_max	T_1/2	AUC_last	AUC_inf	MRT_last	F	CL	V_ss	C₀
Mice^[1]	2 mg/kg	i.v.	/	/	0.515 h	1.88 μM·h	1.88 μM·h	0.283 h	/	21.9 mL/min/kg	0.378 L/kg	8.40 μM
Mice^[1]	10 mg/kg	i.p.	0.250 h	6.10 μM	0.721 h	7.31 μM·h	7.21 μM·h	0.937 h	77.7 %	/	/	/

Chemical Information

No. CAS 2757045-94-4
Appearance Solid
Peso molecular 809.27
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

View the Complete Stock Solution Preparation Table

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].

In Vivo Dissolution Calculator

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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

Protocolo

All Animals and Diseases

Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 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)
Elemental Analysis Report (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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Nowak RP, et al. Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag. Journal of medicinal chemistry. 2021 Aug 12;64(15):11637-11650. [Content Brief]

Calculators

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Calculadora de dilución

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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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