ANXA3 degrader 1
ANXA3 degrader 1 is a degrader targeting annexin A3 (ANXA3), with DC50 values of 1.32 μM and 3.12 μM in MDA-MB-231 and MDA-MB-468 cells, respectively, and exhibits selective activity against ANXA3 relative to other members of the annexin family. ANXA3 degrader 1 induces selective degradation of ANXA3 via the ubiquitin-proteasome pathway rather than autophagy. ANXA3 degrader 1 can be used for research on triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C30H32N6O2S2
- Molecular Weight:572.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
AnxA3 1.32-3.12 μM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-468 | IC50 |
0.71 μM
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Antiproliferative activity against human MDA-MB-468 triple-negative breast cancer cells assessed via CCK8 assay.
Antiproliferative activity against human MDA-MB-468 triple-negative breast cancer cells assessed via CCK8 assay.
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40013713 |
| MDA-MB-231 | IC50 |
1.05 μM
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Antiproliferative activity against human MDA-MB-231 triple-negative breast cancer cells assessed via CCK8 assay.
Antiproliferative activity against human MDA-MB-231 triple-negative breast cancer cells assessed via CCK8 assay.
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40013713 |
| MDA-MB-468 | DC50 |
3.12 μM
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ANXA3 protein degradation activity in human MDA-MB-468 triple-negative breast cancer cells after 24 h incubation, quantified via Western blot.
ANXA3 protein degradation activity in human MDA-MB-468 triple-negative breast cancer cells after 24 h incubation, quantified via Western blot.
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40013713 |
| MDA-MB-231 | DC50 |
1.32 μM
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ANXA3 protein degradation activity in human MDA-MB-231 triple-negative breast cancer cells after 24 h incubation, quantified via Western blot.
ANXA3 protein degradation activity in human MDA-MB-231 triple-negative breast cancer cells after 24 h incubation, quantified via Western blot.
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40013713 |
In Vitro
ANXA3 degrader 1 (18a5) (0.0625-1 μM; 60 s binding, 90 s dissociation) binds to purified ANXA3 protein with a Kd of 0.08 μM[1].
ANXA3 degrader 1 (50 μM; 15-30 min) binds to purified ANXA3 protein, increasing its melting temperature by 1.88 °C[1].
ANXA3 degrader 1 (100 μM) binds to purified ANXA3 protein with a KD of 0.16 μM[1].
ANXA3 degrader 1 (0.5-10 μM; 24 h) induces concentration-dependent degradation of ANXA3 protein in MDA-MB-468 and MDA-MB-231 TNBC cells with DC50 values of 3.12 μM and 1.32 μM, respectively[1].
ANXA3 degrader 1 (18a5) inhibits proliferation of MDA-MB-468 and MDA-MB-231 TNBC cells with IC50 values of 0.71 μM and 1.05 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468, MDA-MB-231 TNBC cell lines
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Concentration:0.5, 1, 2, 4, 6 μM (MDA-MB-231); 1, 3, 6, 8, 10 μM (MDA-MB-468)
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Incubation Time:24 h
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Result:Reduced ANXA3 protein levels in MDA-MB-468 cells to 11% of vehicle control at 10 μM, with a degradation half-maximal effective concentration DC50 = 3.12 μM.
Reduced ANXA3 protein levels in MDA-MB-231 cells to 19% of vehicle control at 6 μM, with a DC50 = 1.32 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C (female, 4-6 weeks of age)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 21 days
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Result:Achieved tumor growth inhibition rates of 65%, 72%, and 96% at doses of 5 mg/kg, 10 mg/kg, and 20 mg/kg, respectively.
Significantly reduced ANXA3 protein expression in tumor tissues in a dose-dependent manner, with notable degradation observed at the 20 mg/kg dose.
Caused no significant weight loss or organ toxicity compared to the control group.
Chemical Information
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Molecular Weight 572.74
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Formula C30H32N6O2S2
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SMILES
CC(C)N1C2=CC=CC=C2C(C3=CC=CC=C3)=NC(NC(SCC(N4CCN(C5=NC=CC=C5)CC4)=O)=S)C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ANXA3 degrader 1 Related Classifications
HY-168950 Related Classifications
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