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).
(Pink: Androgen Receptor Target protein ligand; Blue: 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.
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
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.
-
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.
| 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.
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)