化合物 LY3009120|T6882|TargetMol

LY3009120
1454682-72-4

￥452 2mg 起订

￥697 5mg 起订

￥1134 10mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 LY3009120

英文名称：: LY3009120

CAS号：: 1454682-72-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T6882

Product Introduction

Bioactivity

名称	LY3009120
描述	LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.
细胞实验	Brie?y, cells are grown in DMEM high glucose supplemented with 10% characterized fetal bovine serum and 1% penicillin/streptomycin/L -glutamine at 37℃, 5% CO2, and 95% humidity. Cells are allowed to expand until 70-95% con?uency. A serial dilution of test compound is dispensed into a 384-well black clear bottom plate. 625 cells are added per well in 50 μL of complete growth medium. Plates are incubated for 67 h at 37℃, 5% CO2 , and 95% humidity. Then, 10 μL of a 440 μM solution of resazurin in PBS is added to each well of the plate and plates are incubated for an additional 5 h at 37℃, 5% CO2, and 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nm and an emission of 600 nm. Data are analyzed using Prism software to calculate IC 50 values.(Only for Reference)
激酶实验	Kinase activity measurement using KiNativ assays: Compounds are screened in A375 cell lysates using the ATP-based probe at 5 μM. IC50 values are reported in micromolar units. Cell pellets are resuspended in four volumes of lysis buffer [25 mM Tris pH 7.6, 150 mM NaCl, 1% CHAPS, 1% Tergitol NP-40 type, 1% v/v phosphatase inhibitor cocktail II], sonicated using a tip sonicator, and dounce homogenized. Lysates are cleared by centrifugation at 100,000 g for 30 min. The cleared lysates are filtered through a 0.22 μM syringe filter, and gel filtered into reaction buffer [20 mM Hepes pH 7.8, 150 mM NaCl, 0.1% triton X-100, 1% v/v phosphatase inhibitor cocktail II]. MnCl2 is then added to the lysate to a final concentration of 20 mM prior to inhibitor treatment and probe labeling. Final inhibitor concentrations used for IC50 determinations are 10, 1, 0.1, and 0.01 μM. ATP competition experiments are performed at 1,000, 100, 10, and 1 μM ATP. All inhibitor treatments are performed at room temperature.
动物实验	Animal Models: Female NIH nude rats bearing BRAF V600E ST019VR PDX tumorsFormulation: 20% cyclodextrin, 25 mM phosphate, pH2.0Dosages: 30 mg/kgAdministration: p.o.[1]
体外活性	LY3009120抑制A375细胞和HCT116细胞的生长，其IC50分别为9.2 μM和220 μM。同时，LY3009120也对酪氨酸激酶KDR有抑制作用，其IC50为3.9 μM。[1]
体内活性	在携带BRAF V600E ST019VR PDX肿瘤的大鼠中，LY3009120 (15或30 mg/kg, p.o.)表现出剂量依赖性的肿瘤生长抑制效果。在裸鼠植入A375异种移植瘤中，单次口服LY3009120 (3到50 mg/kg, p.o.)显示出对磷酸化ERK的剂量依赖性抑制，其中抑制磷酸化ERK 50%所需剂量(EC50)为4.36 mg/kg，达到抑制磷酸化ERK 50%的血浆浓度(EC50)为68.9 ng/mL或165 nM。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 10 mg/mL (23.56 mM)
关键字	Raf kinases \| LY3009120 \| DP 4978 \| inhibit \| Autophagy \| LY 3009120 \| LY-3009120 \| Raf \| DP4978 \| Inhibitor
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DP-4978|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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