2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  3. PROTACs Estrogen Receptor/ERR Apoptosis
  4. PROTAC ERα Degrader-4

PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

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

PROTAC ERα Degrader-4 Chemical Structure

PROTAC ERα Degrader-4 Chemical Structure

CAS No. : 2521299-80-7

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PROTAC ERα Degrader-4 Related Antibodies

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Description

PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

IC50 & Target[1]

ERα

5.08 μM (Ki)

ERβ

26.20 μM (Ki)

In Vitro

PROTAC ERα Degrader-4 (1 μM, 12 hours) exhibits significant degradation activity for ERα in MCF-7cells[1].
PROTAC ERα Degrader-4 (2 μM, 12 hours) can degrade wild-type ERα inT47D cells and mutant ERα in T47DD538G and T47DY537S cells[1].
PROTAC ERα Degrader-4 (0.01-10 μM, 72 hours) has inhibitory activity of ERα in Tamoxifen (HY-13757A) -sensitive MCF-7 cells, with the IC50 value of 0.05 μM[1].
PROTAC ERα Degrader-4 (1-10 μM, 72 hours) induce apoptosis and cell cycle arrest of MCF-7 cells[1].
PROTAC ERα Degrader-4 (0.01-10 μM, 12 hours) efficiently degrades ERα protein in the range of 0.01 to10 μM in MCF-7 cell line[1].

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

PROTAC ERα Degrader-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 72 hours
Result: Had inhibitory activity in Tamoxifen-sensitive MCF-7 cells, with the IC50 value of 0.05 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1.0 μM, 5 μM, 5.0 μM
Incubation Time: 72 hours
Result: Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 72 hours
Result: Induced cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 12 hours
Result: Efficiently degraded ERα protein in the range of 0.01 to10 μM, whereas ERα protein levels recovered slightly at a high concentration of 10 μM
In Vivo

PROTAC ERα Degrader-4 (Compound ZD12) (5 μM/kg for i.p., once every 2 days) exhibits potent antitumor activity and ERα degradation effect in tumor tissues in LCC2 orthotopic xenograft tumor models[1].
PROTAC ERα Degrader-4 (5 mg/kg for i.v.) shows a T1/2 of 4.61 h and CL of 64.4 mL/min/kg[1].

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

Animal Model: LCC2 orthotopic xenograft tumor models[1]
Dosage: 5 μM/kg
Administration: Intravenous injection (i.p.)
Result: Exhibited potent antitumor activity and ERα degradation effect in tumor tissues.
Animal Model: BALB/C female mice (Pharmacokinetic assay)[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: Intravenous injection (i.v.); Oral gavage (p.o.)
Result: Pharmacokinetic parameters for PROTAC ERα Degrader-4 (Compound ZD12) in BALB/C female mice [1]
ND: not detected.
Route Dose (mg/kg) CL (mL/min/kg) Tmax (h) T1/2 (h) Cmax (ng/mL) AUC (h•ng/mL)
i.v. 5 64.4 0.08 4.61 3635.73 1342
p.o. 20 ND ND ND ND ND
Molecular Weight

1074.23

Formula

C55H62F3N5O10S2
CAS No.
SMILES

CC1=C(C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@@H](NC(CCCCCOC4=CC=C(C=C4)N(CC(F)(F)F)S(C5C[C@@H]6C(C7=CC=C(C=C7)O)=C([C@H]5O6)C8=CC=C(C=C8)O)(=O)=O)=O)C(C)(C)C)=O)O)=O)C)SC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC ERα Degrader-4 Related Classifications

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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.

Keywords:

PROTAC ERα Degrader-42521299-80-7PROTAC ERα Degrader4PROTAC ERα Degrader 4PROTACsEstrogen Receptor/ERRApoptosisPROTAC ERα DegraderMCF-7primary astrocytesER-positive breast cancerxenograft tumor modelsInhibitorinhibitorinhibit

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