country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Referencia número: HY-145226

Copy Link Print Information

XY-06-007

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

Revisión del cliente

Based on 1 Customer Validation

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: 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

Tamaño

Precio

Stock

Cantidad

Amount: USD 0.00

* Seleccione Cantidad antes de agregar artículos.

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
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

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: 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.

Related Protocols :

Genotoxicity/Mutagenicity Study

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

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Obtener un presupuesto En stock

Other size

Obtener un presupuesto