AZD4877
Based on 1 Customer Validation
AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity.
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。
- 純度: 99.49%
- CAS 番号: 758722-49-5
- 分子式: C28H33N5O2S
- 分子量:503.66
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Cytoskeleton Compound Library
HY-L060
-
Pain-Related Compound Library
HY-L139
-
Cell Death Library
HY-L162
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
Kinesin アイソフォーム固有の製品をすべて表示
More
生物活性
IC50: 2 nM (Eg5)[5]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| COLO 205 | IC50 |
0.002 μM
Compound: 65
|
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
|
[PMID: 21899292] |
| COLO 205 | IC50 |
0.003 μM
Compound: 1, AZD-4877
|
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
Anticancer activity against human COLO205 cells after 72 hrs by MTS/PMS assay
|
[PMID: 21899292] |
AZD4877 (10 nM, 24 or 48 hours) induces apoptosis in human bladder cancer cells and AZD4877-sensitive cells generally expressed high levels of p63[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:UC1, UC3, UC6, UC12, UC15, RT4,JB,BV, T24 cell line
-
Concentration:10 nM
-
Incubation Time:24 or 48 hours
-
Result:Induced apoptosis in human bladder cancer cells
AZD4877 (i.v., 6 mg/kg; single dose) shows a T1/2 of 3.5 h, and CL of 36 mL/min/kg in Hans Wistar rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 758722-49-5
-
性状 Solid
-
分子量 503.66
-
分子式 C28H33N5O2S
-
Color Off-white to light yellow
-
SMILES
O=C(N(C(C(C)C)C1=NC2=C(C(N1CC3=CC=CC=C3)=O)C(C)=NS2)CCCN)C4=CC=C(C)C=C4
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (99.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (9.93 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (277 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Theoclitou ME, et.al. Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent. J Med Chem. 2011 Oct 13;54(19):6734-50. [Content Brief]
[2]. Marquis L, et.al. p63 expression correlates with sensitivity to the Eg5 inhibitor ZD4877 in bladder cancer cells. Cancer Biol Ther. 2012 May;13(7):477-86. [Content Brief]
[3]. Gerecitano JF, et.al. A Phase I trial of the kinesin spindle protein (Eg5) inhibitor AZD4877 in patients with solid and lymphoid malignancies. Invest New Drugs. 2013 Apr;31(2):355-62. [Content Brief]
[4]. Shahin R, et.al. Kinesin spindle protein inhibitors in cancer: from high throughput screening to novel therapeutic strategies. Future Sci OA. 2022 Feb 21;8(3):FSO778. [Content Brief]
[5]. Myers SM, et.al. Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy. Future Med Chem. 2016;8(4):463-89. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9855 mL | 9.9273 mL | 19.8547 mL | 49.6367 mL |
| 5 mM | 0.3971 mL | 1.9855 mL | 3.9709 mL | 9.9273 mL | |
| 10 mM | 0.1985 mL | 0.9927 mL | 1.9855 mL | 4.9637 mL | |
| 15 mM | 0.1324 mL | 0.6618 mL | 1.3236 mL | 3.3091 mL | |
| 20 mM | 0.0993 mL | 0.4964 mL | 0.9927 mL | 2.4818 mL | |
| 25 mM | 0.0794 mL | 0.3971 mL | 0.7942 mL | 1.9855 mL | |
| 30 mM | 0.0662 mL | 0.3309 mL | 0.6618 mL | 1.6546 mL | |
| 40 mM | 0.0496 mL | 0.2482 mL | 0.4964 mL | 1.2409 mL | |
| 50 mM | 0.0397 mL | 0.1985 mL | 0.3971 mL | 0.9927 mL | |
| 60 mM | 0.0331 mL | 0.1655 mL | 0.3309 mL | 0.8273 mL | |
| 80 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6205 mL |
AZD4877 関連分類
HY-13224 関連分類
Powered by Bioz