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SAR439859 

Cat. No.: HY-133017 Purity: 99.25%
Handling Instructions

SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer.

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

SAR439859 Chemical Structure

SAR439859 Chemical Structure

CAS No. : 2114339-57-8

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5 mg USD 380 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2350 In-stock
Estimated Time of Arrival: December 31
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Description

SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation[1]. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer[2].

IC50 & Target[1]

ERα

0.2 nM (EC50)

In Vitro

SAR439859 (compound 43d) induces strong in vivo antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations[1].

In Vivo

SAR439859 (compound 43d; orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID[1].
SAR439859 (3 mg/kg for iv and 10 mg/kg for po) shows a low to moderate clearance in the three animal species tested (0.03-1.92 L/h•kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species. It is noticed that T1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog)[1].

Animal Model: Nu/nu mouse with MCF7 tumor xenograft model[1]
Dosage: 2.5, 5, 12.5, 25 mg/kg
Administration: Orally; twice daily for 30 days
Result: Exhibited substantial tumor-growth inhibition and displayed tumor regression at the dose of 25 mg/kg/BID.
Animal Model: Mouse, rat and dog[1]
Dosage: 3 mg/kg (iv) and 10 mg/kg (po) (Pharmacokinetic Analysis)
Administration: Iv or po
Result: Showed a low to moderate clearance in the three animal species tested (0.03-1.92 L/h•kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species.
Clinical Trial
Molecular Weight

554.48

Formula

C₃₁H₃₀Cl₂FNO₃

CAS No.

2114339-57-8

SMILES

O=C(C1=CC=C(C(C2=CC=C(O[[email protected]@H]3CN(CCCF)CC3)C=C2)=C(C4=CC=C(Cl)C=C4Cl)CCC5)C5=C1)O

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 : 125 mg/mL (225.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8035 mL 9.0175 mL 18.0349 mL
5 mM 0.3607 mL 1.8035 mL 3.6070 mL
10 mM 0.1803 mL 0.9017 mL 1.8035 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (3.75 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.75 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.75 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

SAR439859SAR 439859SAR-439859Estrogen Receptor/ERROrallynonsteroidaldegraderSERDERdegradationantitumorcross-resistancebreastcancerInhibitorinhibitorinhibit

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SAR439859
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HY-133017
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