CCT251236
目录号 : GC19094An inhibitor of Hsf1-mediated transcription
Cas No.:1693731-40-6
Sample solution is provided at 25 µL, 10mM.
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CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
CCT251236 displays the desired balance of in vitro properties, while maintaining excellent cellular activity with an IC50 of 19 nM. The free GI50 in SK-OV-3 cells is 1.1 nM. Western blotting confirms that CCT251236 blocks the HSF1-mediated induction of both HSP72 and HSP27 as representative heat shock proteins, following treatment with the HSP90 inhibitor 17AAG. Also, qPCR analysis demonstrates that CCT251236 inhibits the induction of HSP72 at the mRNA level, clearly blocking the induction of HSPA1A gene expression with an IC50 of 40 nM[1].
CCT251236 possesses low total blood clearance (10% hepatic blood flow) and moderate oral bioavailability, with a half-life sufficient to allow once-a-day dosing. Clear therapeutic efficacy is observed with CCT251236, with a tumor growth inhibition of 70% based on final tumor volumes[1].
References:
[1]. Cheeseman MD, et al. Discovery of a Chemical Probe Bisamide (CCT251236): An OrallyBioavailable Efficacious Pirin Ligand from a Heat ShockTranscription Factor 1 (HSF1) Phenotypic Screen. J Med Chem. 2017 Jan 12;60(1):180-201.
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Animal experiment: |
Mice: SK-OV-3 cells are injected subcutaneously into athymic mice for tumor formation. Once tumors are established, the mice are randomized into treatment and control groups and are dosed orally once-a-day with either vehicle or 20 mg/kg of CCT251236. Tumor volumes and mouse body weights are measured throughout and tumor weights are measured at the end of the study, while total tumor concentrations are measured 2 and 6 hours post final dose[1]. |
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References: [1]. Cheeseman MD, et al. Discovery of a Chemical Probe Bisamide (CCT251236): An OrallyBioavailable Efficacious Pirin Ligand from a Heat ShockTranscription Factor 1 (HSF1) Phenotypic Screen. J Med Chem. 2017 Jan 12;60(1):180-201. |
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| Cas No. | 1693731-40-6 | SDF | |
| 化学名 | N-[5-[[(2,3-dihydro-1,4-benzodioxin-6-yl)carbonyl]amino]-2-methylphenyl]-2-[2-(1-pyrrolidinyl)ethoxy]-6-quinolinecarboxamide | ||
| Canonical SMILES | CC1=CC=C(NC(C2=CC(OCCO3)=C3C=C2)=O)C=C1NC(C4=CC(C=CC(OCCN5CCCC5)=N6)=C6C=C4)=O | ||
| 分子式 | C32H32N4O5 | 分子量 | 552.62 |
| 溶解度 | 3mg/mL in DMSO, or in DMF | 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 | 1.8096 mL | 9.0478 mL | 18.0956 mL |
| 5 mM | 0.3619 mL | 1.8096 mL | 3.6191 mL |
| 10 mM | 0.181 mL | 0.9048 mL | 1.8096 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet