2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Androgen Receptor
  4. A031

A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP).

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A031 Chemical Structure

A031 Chemical Structure

CAS No. : 2682255-44-1

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A031 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP)[1].

In Vitro

A031 (0.125-1.000 μM) shows inhibition to AR with an IC50 value less than 0.25 μM[1].
A031 (2 μM; 2-4.5 h) reduces the AR protein level in VCaP cell lines[1].

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

A031 Related Antibodies

Western Blot Analysis[1]

Cell Line: VCaP cell lines
Concentration: 2 μM
Incubation Time: 2, 3.5 and 4.5 hours
Result: Reduced the AR protein level, and AR proteins was almost degraded after 4.5 h treatment.
In Vivo

A031 (2.8, 8.3 and 25 μM; in culture solution for 5 days) inhibits prostate cancer growth in zebrafish[1].
1.19 Pharmacokinetic Properties of A031 in Rats[1].

Rats
IV 1 mg/kg
t1/2 (h) 0.57
Cmax (ng/mL) 14366.2
AUClast (h·ng/mL) 1773.8
AUCINF_pred (h·ng/mL) 1773.8
Vz_pred (L/kg) 0.47
Cl_pred (L/h/kg) 0.57

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

Animal Model: Wild type AB strain zebrafish with human prostate cancer (VCap) cells transplantatio[1]
Dosage: 2.8, 8.3 and 25 μM
Administration: Aqueous solution culture, at 35℃, for 5 days
Result: Inihibited tumor growth with growth inhibition rates of 28%, 55% and 61% at 2.8, 8.3 and 25 μM, respectively.
Molecular Weight

981.60

Formula

C50H61ClN10O7S
CAS No.
SMILES

O=C(N([C@@H]1C2)[C@H](CC1)C[C@@H]2OC3=CC(Cl)=C(C=C3)C#N)C4=CN=C(N5CCN(CC5)CCOCC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(N[C@H](C7=CC=C(C8=C(N=CS8)C)C=C7)C)=O)=O)=O)N=C4
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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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A031 Related Classifications

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

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× = ×
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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:

A0312682255-44-1A 031A-031PROTACsAndrogen ReceptorPROTACzebrafishdegraderVCaPInhibitorinhibitorinhibit

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