A031

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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).

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

A031 Chemical Structure

CAS No. : 2682255-44-1

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Biological Activity
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Description

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.

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
t_1/2 (h)	0.57
C_max (ng/mL)	14366.2
AUC_last (h·ng/mL)	1773.8
AUC_{INF_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.

2682255-44-1

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

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

Handling Instructions (2659 KB)

References

[1]. Chen L, et al. Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer. Eur J Med Chem. 2021 Apr 15;216:113307. [Content Brief]

A031 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:

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

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