LY2874455

产品编号 T2361Cas号 1254473-64-7

别名 LY 2874455|||LY-2874455

LY2874455 是pan-FGFR 抑制剂，能够抑制FGFR1 (IC50:2.8 nM)，FGFR2 (IC50:2.6 nM)，FGFR3 (IC50:6.4 nM)，FGFR4 (IC50:6 nM)。

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LY2874455

产品编号 T2361别名 LY 2874455, LY-2874455Cas号 1254473-64-7

LY2874455 是pan-FGFR 抑制剂，能够抑制FGFR1 (IC50:2.8 nM)，FGFR2 (IC50:2.6 nM)，FGFR3 (IC50:6.4 nM)，FGFR4 (IC50:6 nM)。

规格	价格	库存
1 mg	¥ 366	现货
2 mg	¥ 523	现货
5 mg	¥ 828	现货
10 mg	¥ 1,230	现货
25 mg	¥ 2,260	现货
50 mg	¥ 3,730	现货
100 mg	¥ 4,990	现货
1 mL x 10 mM (in DMSO)	¥ 913	现货

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产品介绍

生物活性

产品描述	LY2874455 has been used in trials studying the treatment of Advanced Cancer.
靶点活性	FGFR4:6 nM, FGFR3:6.4 nM, FGFR1:2.8 nM, FGFR2:2.6 nM, VEGFR2:7 nM
体外活性	在携带RT-112,OPM-2（DSMZ）,SNU-16或NCI-H460异种移植物的小鼠中,LY2874455（3 mg/kg,口服）导致肿瘤生长的剂量依赖性抑制.LY2874455在小鼠心脏组织中,表现出对FGF诱导的Erk磷酸化的有效抑制,TED50和TED90值分别为1.3 和 3.2 mg/kg.
体内活性	LY2874455在KMS-11,OPM-2,SNU-16和KATO-III细胞中显示FGFR依赖性抗增殖作用。在RT-112细胞,HUVECs,KATO-III细胞和SNU-16细胞中,LY2874455抑制FGF/FGFR介导的信号传导活性。
激酶实验	Biochemical filter-binding assays for detection of FGFR phosphorylation activities : Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader.
细胞实验	Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). (Only for Reference)
别名	LY 2874455, LY-2874455

偶联与修饰

抗原信息

存储 & 运输

化学信息

分子量	444.31
分子式	C₂₁H₁₉Cl₂N₅O₂
CAS No.	1254473-64-7

储存&溶解度

存储

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

溶解度信息

DMSO: 82 mg/mL (184.6 mM)

Ethanol: 53 mg/mL (119.3 mM)

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2507 mL	11.2534 mL	22.5068 mL	112.5340 mL
5 mM	0.4501 mL	2.2507 mL	4.5014 mL	22.5068 mL
10 mM	0.2251 mL	1.1253 mL	2.2507 mL	11.2534 mL
20 mM	0.1125 mL	0.5627 mL	1.1253 mL	5.6267 mL
50 mM	0.0450 mL	0.2251 mL	0.4501 mL	2.2507 mL
100 mM	0.0225 mL	0.1125 mL	0.2251 mL	1.1253 mL