LY3039478
(Synonyms: LY3039478) 目录号 : GC12653
A Notch inhibitor
Cas No.:1421438-81-4
Sample solution is provided at 25 µL, 10mM.
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LY3039478 is a novel and potent Notch inhibitor with IC50 of 0.41 nM.
The novel and unique Notch Inhibitor, LY3039478, has progressed into clinical development by Lilly co. ltd. LY3039478 displays the best overall profile and is unique within the SAR investigated. LY3039478 Displays Interesting Atropisomer Phenomena. The average LY3039478 major/minor rotational isomer ratio ranged between 14 and 28 in plasma. The crystalline monohydrate form of LY3039478 consists of a single rotational isomer and is chemically and physically stable for at least 14 days under accelerated stability test conditions.
Reference:
[1].Warren J. Porter. Discovery of a Novel Notch Inhibitor. The 8th SCI-RSC Symposium on Proteinase Inhibitor Design April 15-16, 2013, Basel, Switzerland.
| Cell experiment [1]: | |
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Cell lines |
Normal human kidney tubular epithelial cell line HK2 and renal cell cancer cell lines 786-O, 769-P and Caki |
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Preparation method |
The solubility of this compound in DMSO is >23.2 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0-10 μM |
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Applications |
LY3039478 was found to be able to significantly inhibit the growth of two CCRCC cell lines in a concentration dependent manner. LY3039478 treatment also led to decreased expression of Myc and Cyclin A1, two genes that were part of the NOTCH driven proliferative signature in murine and human model systems. LY3039478 treatment also led to G0/G1 cell cycle arrest in CCRCC cells. |
| Animal experiment [1]: | |
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Animal models |
NSG xenograft mice model with 769-P CCRCC cells |
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Dosage form |
8 mg/kg by oral gavage |
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Application |
LY3039478 treatment resulted in significantly increased survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Bhagat TD et al.Notch Pathway Is Activated via Genetic and Epigenetic Alterations and Is a Therapeutic Target in Clear Cell Renal Cancer. J Biol Chem. 2017 Jan 20;292(3):837-846. | |
| Cas No. | 1421438-81-4 | SDF | |
| 别名 | LY3039478 | ||
| 化学名 | 4,4,4-trifluoro-N-[(2S)-1-[[(7S)-5-(2-hydroxyethyl)-6-oxo-7H-pyrido[2,3-d][3]benzazepin-7-yl]amino]-1-oxopropan-2-yl]butanamide | ||
| Canonical SMILES | CC(C(=O)NC1C2=CC=CC=C2C3=C(N=CC=C3)N(C1=O)CCO)NC(=O)CCC(F)(F)F | ||
| 分子式 | C22H23F3N4O4 | 分子量 | 464.44 |
| 溶解度 | ≥ 23.2 mg/mL in DMSO, ≥ 89.4 mg/mL in EtOH with ultrasonic | 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 | 2.1531 mL | 10.7657 mL | 21.5313 mL |
| 5 mM | 0.4306 mL | 2.1531 mL | 4.3063 mL |
| 10 mM | 0.2153 mL | 1.0766 mL | 2.1531 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet