1. Vitamin D Related/Nuclear Receptor PROTAC
  2. Estrogen Receptor/ERR PROTACs
  3. AZ'6421

AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.

For research use only. We do not sell to patients.

AZ'6421 Chemical Structure

AZ'6421 Chemical Structure

CAS No. : 2361115-35-5

Size Price Stock Quantity
1 mg USD 640 In-stock
5 mg USD 1600 In-stock
10 mg USD 2560 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer[1].

IC50 & Target

IC50: 0.6 nM (ER binding); 0.4 nM (ER degradation)[1]

In Vitro

AZ'6421 (example 72) exhibits anti-tumour activity via the ability to degrade the estrogen receptor in a number of different breast cancer cell-lines (MCF-7, CAMA-I, and BT474)[1].
AZ'6421 (0.3 μM) has ER binding and ER degradation with IC50 values of 0.6 nM and 0.4 nM, respectively in MCF-7 cell lines[1].

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

Molecular Weight

975.17

Formula

C52H65F3N6O7S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H](N1CC(C)(F)C)CC2=C(NC3=C2C=CC=C3)[C@H]1C4=C(F)C=C(OCCCOCCCOCC(N[C@@H](C(C)(C)C)C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)=O)C=C4F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (102.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0255 mL 5.1273 mL 10.2546 mL
5 mM 0.2051 mL 1.0255 mL 2.0509 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0255 mL 5.1273 mL 10.2546 mL 25.6366 mL
5 mM 0.2051 mL 1.0255 mL 2.0509 mL 5.1273 mL
10 mM 0.1025 mL 0.5127 mL 1.0255 mL 2.5637 mL
15 mM 0.0684 mL 0.3418 mL 0.6836 mL 1.7091 mL
20 mM 0.0513 mL 0.2564 mL 0.5127 mL 1.2818 mL
25 mM 0.0410 mL 0.2051 mL 0.4102 mL 1.0255 mL
30 mM 0.0342 mL 0.1709 mL 0.3418 mL 0.8546 mL
40 mM 0.0256 mL 0.1282 mL 0.2564 mL 0.6409 mL
50 mM 0.0205 mL 0.1025 mL 0.2051 mL 0.5127 mL
60 mM 0.0171 mL 0.0855 mL 0.1709 mL 0.4273 mL
80 mM 0.0128 mL 0.0641 mL 0.1282 mL 0.3205 mL
100 mM 0.0103 mL 0.0513 mL 0.1025 mL 0.2564 mL
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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.

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Product Name:
AZ'6421
Cat. No.:
HY-135312
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