| CAS NO: | 959763-06-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 1mg | 电议 |
| 5mg | 电议 |
| Cas No. | 959763-06-5 |
| 别名 | 4-[[4-氨基-6-(5-氯-1H,3H-萘并[1,8-CD]吡喃-6-基)-1,3,5-三嗪-2-基]硫基]丁酰胺 |
| Canonical SMILES | ClC1=C(C2=NC(N)=NC(SCCCC(N)=O)=N2)C3=CC=CC4=C3C(COC4)=C1 |
| 分子式 | C19H18Cl N5O2S |
| 分子量 | 415.9 |
| 溶解度 | ≥ 19.95mg/mL in DMSO |
| 储存条件 | Desiccate at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | CH5138303 is an inhibitor of Hsp90 with Kd value of 0.48 nM [1]. Heat shock protein 90 (HSP90) is a chaperone protein that stabilizes proteins against heat stress, assists proteins to fold properly and aids in protein degradation. Also, HSP90 stabilizes proteins required for tumor growth. CH5138303 is an orally available Hsp90 inhibitor. CH5138303 showed improved water solubility with 646 μM and high affinity against Hsp90α with Kd value of 0.48 nM. In NCI-N87 cells, CH5138303 decreased the protein level and phosphorylation of Hsp90 target proteins such as Raf1, AKT, EGFR and HER2 [1]. In mice, CH5138303 exhibited high plasma clearance, oral bioavailability and total systemic exposure (AUC). In mice bearing human NCI-N87 gastric cancer xenograft model, CH5138303 exhibited potent antitumor efficacy with tumor growth inhibition (TGI) of 136% and ED50 value of 3.9 mg/kg [1]. Reference: |
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