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  3. ARV-471

ARV-471 

Cat. No.: HY-138642 Purity: 99.60%
Handling Instructions

ARV-471 is an oral estrogen receptor PROTAC protein degrader for breast cancer. ARV-471 is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. ARV-471 leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM.

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

ARV-471 Chemical Structure

ARV-471 Chemical Structure

CAS No. : 2229711-68-4

Size Price Stock Quantity
5 mg USD 980 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
25 mg USD 3450 In-stock
Estimated Time of Arrival: December 31
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

ARV-471 is an oral estrogen receptor PROTAC protein degrader for breast cancer. ARV-471 is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. ARV-471 leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM[1].

IC50 & Target

Estrogen receptor[1]

Clinical Trial
Molecular Weight

723.90

Formula

C45H49N5O4

CAS No.
SMILES

O=C([[email protected]@H](N(CC1=C2C=CC(N3CCN(CC4CCN(C5=CC=C([[email protected]]6[[email protected]@H](C7=CC=CC=C7)CCC8=C6C=CC(O)=C8)C=C5)CC4)CC3)=C1)C2=O)CC9)NC9=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (151.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3814 mL 6.9070 mL 13.8141 mL
5 mM 0.2763 mL 1.3814 mL 2.7628 mL
10 mM 0.1381 mL 0.6907 mL 1.3814 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5.5 mg/mL (7.60 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (2.76 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (2.76 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MCE.
References

Purity: 99.60%

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Product Name:
ARV-471
Cat. No.:
HY-138642
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