RTC-5
(Synonyms: TRC-382) 目录号 : GC37568
RTC-5 是一种具有抗癌效力的优化吩噻嗪。RTC-5 显示针对 EGFR 驱动的癌症的异种移植模型的功效，其效果归因于 PI3K-AKT 和 RAS-ERK 信号传导的负调节。
Cas No.:1423077-49-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling[1]. IC50: EGFR[1]
RTC-5 (0-40 μM; 48 hours) inhibits H1650 lung adenocarcinoma cell growth with an GI50 of 12.6μM[1].RTC-5 (20-40 μM; 24 hours) negatively regulates PI3K-AKT and RAS-ERK pathways by decreasing phospho-AKT and phospho-ERK levels expression[1]. Cell Viability Assay[1] Cell Line: H1650 lung adenocarcinoma cells
[1]. Kastrinsky DB, et al. Reengineered tricyclic anti-cancer agents. Bioorg Med Chem. 2015 Oct 1;23(19):6528-34.
| Cas No. | 1423077-49-9 | SDF | |
| 别名 | TRC-382 | ||
| Canonical SMILES | O=S(C1=CC=C(OC(F)(F)F)C=C1)(NCCCN2C3=CC(Cl)=CC=C3CCC4=CC=CC=C42)=O | ||
| 分子式 | C24H22ClF3N2O3S | 分子量 | 510.96 |
| 溶解度 | DMSO: 15 mg/mL (29.36 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9571 mL | 9.7855 mL | 19.571 mL |
| 5 mM | 0.3914 mL | 1.9571 mL | 3.9142 mL |
| 10 mM | 0.1957 mL | 0.9786 mL | 1.9571 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Reengineered tricyclic anti-cancer agents
Bioorg Med Chem 2015 Oct 1;23(19):6528-34.PMID:26372073DOI:PMC8293910
The phenothiazine and dibenzazepine tricyclics are potent neurotropic drugs with a documented but underutilized anti-cancer side effect. Reengineering these agents (TFP, CPZ, CIP) by replacing the basic amine with a neutral polar functional group (e.g., RTC-1, RTC-2) abrogated their CNS effects as demonstrated by in vitro pharmacological assays and in vivo behavioral models. Further optimization generated several phenothiazines and dibenzazepines with improved anti-cancer potency, exemplified by RTC-5. This new lead demonstrated efficacy against a xenograft model of an EGFR driven cancer without the neurotropic effects exhibited by the parent molecules. Its effects were attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.