A031
A031 is a PROTAC degrader targeting the androgen receptor. A031 induces time-dependent degradation of androgen receptor protein. A031 exerts tumor growth inhibitory effects in a zebrafish model xenografted with human prostate cancer cells. A031 can be used in studies related to prostate cancer.
(Pink: Androgen Receptor ligand (HY-175937); Blue: VHL and VHL ligand (HY-112078); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2682255-44-1
- 分子式: C50H61ClN10O7S
- 分子量:981.60
-
保管条件:
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]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
体外実験
A031 (2.0 μM; 2-4.5 h) induces time-dependent degradation of AR protein in AR-positive human prostate cancer VCaP cells, with near-complete degradation observed after 4.5 h of treatment with 2.0 μM A031[1].
A031 (2.0 μM) acts as a bona fide AR degrader in AR-positive human prostate cancer VCaP cells, as its AR-degrading activity is blocked by proteasome and NEDD8 pathway inhibitors but not by VHL-3 pre-treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:AR-positive human prostate cancer VCaP cells
-
Concentration:0.125 μM; 0.25 μM; 0.5 μM; 1.0 μM
-
Incubation Time:4 days
-
Result:Inhibited VCaP cell viability in a dose-dependent manner.
Achieved a cell inhibition rate of 69.56% at 1.0 μM.
Showed a good inhibition rate even at 0.125 μM.
Had an IC50 for cell inhibition of less than 0.25 μM.
-
Cell Line:AR-positive human prostate cancer VCaP cells
-
Concentration:2.0 μM
-
Incubation Time:2 h, 3.5 h, 4.5 h
-
Result:Reduced AR protein levels within 2 h of treatment.
Almost completely degraded AR protein after 4.5 h of treatment.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | AUClast | AUCinf | Vz | CL |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 0.57 h | 14366.2 ng/mL | 1773.8 ng·h/mL | 1773.8 ng·h/mL | 0.47 L/kg | 0.57 L/h/kg |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:wild-type AB strain (2 days post-fertilization)[1]
-
Dosage:2.8 μM; 8.3 μM; 25 μM
-
Administration:static exposure; 2 days
-
Result:Achieved a 28% tumor growth inhibition rate with a tumor fluorescence intensity of 379577 pixels.
Achieved a 55% tumor growth inhibition rate with a tumor fluorescence intensity of 240013 pixels.
Achieved a 61% tumor growth inhibition rate with a tumor fluorescence intensity of 208489 pixels.
-
Animal Model:wild-type AB strain (3 days post-fertilization)[1]
-
Dosage:6.25 μM; 12.5 μM; 25 μM; 50 μM; 100 μM
-
Administration:static exposure; 5 days
-
Result:Caused 0% mortality and no toxic phenotypes at 6.25 μM, 12.5 μM, and 25 μM.
Caused obvious precipitation at 50 μM and 100 μM, with mortality data not reported.
Determined a minimal toxic concentration (MTC) of 25 μM.
化学情報
-
CAS 番号 2682255-44-1
-
分子量 981.60
-
分子式 C50H61ClN10O7S
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
A031 関連分類
HY-148777 関連分類
Powered by Bioz