LY3039478

目录号: GC12653纯度: >98.00%同义词: LY3039478

A Notch inhibitor

Cas No.: 1421438-81-4

规格	价格	库存	数量
1mg	¥400.00	现货	1
5mg	¥827.00	现货	1
10mg	¥1,400.00	现货	1
25mg	¥2,800.00	现货	1
50mg	¥4,019.00	现货	1
10mM (in 1mL DMSO)	¥894.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment [1]:
Cell lines	Normal human kidney tubular epithelial cell line HK2 and renal cell cancer cell lines 786-O, 769-P and Caki
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.
Reacting condition	0-10 μM
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]:
Animal models	NSG xenograft mice model with 769-P CCRCC cells
Dosage form	8 mg/kg by oral gavage
Application	LY3039478 treatment resulted in significantly increased survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC.
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.
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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号

1421438-81-4

同义词

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

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 g/mol

溶解性

≥ 23.2 mg/mL in DMSO, ≥ 89.4 mg/mL in EtOH with ultrasonic

保存条件

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°C，然后在超声波浴中震荡一段时间。

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。

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