Fexagratinib (Synonyms: AZD4547; ADSK091)

目录号: HY-13330 纯度: 99.85%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Fexagratinib (AZD4547; ADSK091) 是一种有效的 FGFR 家族抑制剂，作用于 FGFR1，FGFR2，FGFR3 和 FGFR4，IC₅₀ 分别为 0.2 nM，2.5 nM，1.8 nM 和 165 nM。

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Fexagratinib Chemical Structure

CAS No. : 1035270-39-3

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥818	In-stock
1 mg	￥338	In-stock
5 mg	￥744	In-stock
10 mg	￥1000	In-stock
50 mg	￥2800	In-stock
100 mg	￥4500	In-stock
200 mg	现货	询价
500 mg		询价
1 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Fexagratinib:

Fexagratinib (Standard) 询价

MCE 顾客使用本产品发表的 24 篇科研文献

: Fexagratinib purchased from MCE. Usage Cited in: Front Cell Dev Biol. 2020 May 7;8:287. [Abstract]; Determination in L3.6 cells of FGF2-induced FGFR phosphorylation by Western blot in the presence of AZD4547 . FGFR1 and alpha-Tubulin are used as loading controls.

Fexagratinib 相关产品

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Fexagratinib (AZD4547; ADSK091) is a potent inhibitor of the FGFR family with IC₅₀s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

IC₅₀ & Target^[1]

FGFR1

0.2 nM (IC₅₀)

FGFR2

2.5 nM (IC₅₀)

FGFR3

1.8 nM (IC₅₀)

FGFR4

165 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.062 μM Compound: AZD4547	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25736993]
B16-F10	IC₅₀	0.051 μM Compound: AZD4547	Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay	[PMID: 25736993]
BaF3	IC₅₀	222 nM Compound: 1; AZD-4547	Antiproliferative activity against mouse BAF3 cells expressing VEGFR2 after 72 hrs Antiproliferative activity against mouse BAF3 cells expressing VEGFR2 after 72 hrs	[PMID: 29775937]
BaF3	IC₅₀	339.2 nM Compound: 1; AZD-4547	Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FGFR4 kinase after 72 hrs by CCK8 or MTT assay Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FGFR4 kinase after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
BaF3	IC₅₀	543.5 nM Compound: 1; AZD-4547	Antiproliferative activity against mouse BAF3 cells expressing TEL-fused KDR kinase after 72 hrs by CCK8 or MTT assay Antiproliferative activity against mouse BAF3 cells expressing TEL-fused KDR kinase after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
BGC-823	IC₅₀	7.9 μM Compound: AZD4547	Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 27829519]
DMS-114	IC₅₀	14 nM Compound: AZD4547	Antiproliferative activity against human DMS-114 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay Antiproliferative activity against human DMS-114 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay	[PMID: 36096343]
HeLa 229	IC₅₀	0.14 μM Compound: AZD4547	Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay	[PMID: 25736993]
Huh-7	IC₅₀	> 10 μM Compound: AZD4547	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
Huh-7	IC₅₀	284.3 nM Compound: 1; AZD-4547	Antiproliferative activity against FGF19/FGFR4 expressing human HuH7 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGF19/FGFR4 expressing human HuH7 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
KG-1	IC₅₀	< 0.2 nM Compound: AZD4547	Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
KG-1	IC₅₀	< 0.2 nM Compound: AZD4547	Inhibition of FGFR1 in human KG1 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of FGFR1 in human KG1 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27117427]
KG-1	IC₅₀	1.9 nM Compound: 1; AZD-4547	Antiproliferative activity against human KG1 cells expressing FGFR1 after 72 hrs Antiproliferative activity against human KG1 cells expressing FGFR1 after 72 hrs	[PMID: 29775937]
KG-1	IC₅₀	3.3 nM Compound: AZD4547	Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay	[PMID: 28687204]
KG-1	IC₅₀	3.7 nM Compound: 1; AZD4547	Antiproliferative activity against human KG1 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against human KG1 cells measured after 72 hrs by CCK8 assay	[PMID: 31335138]
KG-1	IC₅₀	5.8 nM Compound: AZD4547	Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay	[PMID: 30572178]
KG-1	IC₅₀	6.4 nM Compound: 5	Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
L02	IC₅₀	18.21 μM Compound: AZD4547	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay	[PMID: 25736993]
MGC-803	IC₅₀	6.2 μM Compound: AZD4547	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 27829519]
NCI-H1581	IC₅₀	0.024 μM Compound: AZD4547	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
NCI-H1581	IC₅₀	15.8 nM Compound: AZ04547	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as reduction in cell viability measured after 72 hrs Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as reduction in cell viability measured after 72 hrs	[PMID: 36802596]
NCI-H1581	IC₅₀	37.9 nM Compound: AZD4547	Antiproliferative activity against human NCI-H1581 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
NCI-H1581	IC₅₀	4 nM Compound: AZD4547	Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay Antiproliferative activity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 120 hrs by MTT assay	[PMID: 36096343]
NCI-H1581	IC₅₀	40 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR1 amplified human NCI-H1581 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR1 amplified human NCI-H1581 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
NCI-H1581	IC₅₀	40 nM Compound: 1; AZD-4547	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 after 72 hrs Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 after 72 hrs	[PMID: 29775937]
NCI-H1581	IC₅₀	92.1 nM Compound: 5	Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
NCI-H460	IC₅₀	> 10 μM Compound: AZD4547	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
NCI-H716	IC₅₀	0.6 nM Compound: AZ04547	Antiproliferative activity against human NCI-H716 cells expressing FGFR2 assessed as reduction in cell viability measured after 72 hrs Antiproliferative activity against human NCI-H716 cells expressing FGFR2 assessed as reduction in cell viability measured after 72 hrs	[PMID: 36802596]
NCI-H716	IC₅₀	5.9 nM Compound: AZD4547	Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay	[PMID: 30572178]
OPM-2	IC₅₀	83.6 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR3 amplified human OPM2 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR3 amplified human OPM2 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
OPM-2	IC₅₀	83.6 nM Compound: AZ04547	Antiproliferative activity against human OPM-2 cells expressing FGFR3 assessed as reduction in cell viability measured after 72 hrs Antiproliferative activity against human OPM-2 cells expressing FGFR3 assessed as reduction in cell viability measured after 72 hrs	[PMID: 36802596]
RT-112	GI₅₀	0.0292 μM Compound: AZD4547	Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay	[PMID: 27599742]
RT-112	IC₅₀	0.6 nM Compound: AZD4547	Antiproliferative activity against human RT112 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human RT112 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
RT-112	IC₅₀	0.6 nM Compound: AZD4547	Inhibition of FGFR3 in human RT112 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of FGFR3 in human RT112 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27117427]
RT-112	IC₅₀	36.4 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR3 amplified human RT112 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR3 amplified human RT112 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
RT-112	IC₅₀	83.8 nM Compound: 1; AZD-4547	Antiproliferative activity against human RT112 cells expressing FGFR3 after 72 hrs Antiproliferative activity against human RT112 cells expressing FGFR3 after 72 hrs	[PMID: 29775937]
RT-112	IC₅₀	88.4 nM Compound: 5	Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
SGC-7901	IC₅₀	2.8 μM Compound: AZD4547	Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay	[PMID: 27829519]
SK-HEP1	IC₅₀	2.78 μM Compound: AZD4547	Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
SNU-16	IC₅₀	0.006 μM Compound: AZD4547	Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay	[PMID: 34129329]
SNU-16	IC₅₀	1.2 nM Compound: AZD4547	Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay	[PMID: 27326339]
SNU-16	IC₅₀	1.5 nM Compound: 1; AZD-4547	Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 or MTT assay Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 or MTT assay	[PMID: 29522671]
SNU-16	IC₅₀	13.4 nM Compound: 5	Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
SNU-16	IC₅₀	19.6 nM Compound: AZD4547	Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay	[PMID: 30572178]
SNU-16	IC₅₀	3.4 nM Compound: AZD4547	Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay	[PMID: 28687204]
SNU-16	IC₅₀	3.6 nM Compound: AZD4547	Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27117427]
SNU-16	IC₅₀	3.7 nM Compound: AZ04547	Antiproliferative activity against human SNU-16 cells assessed as reduction in cell viability measured for 72 hrs Antiproliferative activity against human SNU-16 cells assessed as reduction in cell viability measured for 72 hrs	[PMID: 36802596]
SNU-16	IC₅₀	4.9 nM Compound: 1; AZD4547	Antiproliferative activity against human SNU16 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against human SNU16 cells measured after 72 hrs by CCK8 assay	[PMID: 31335138]
SNU-16	IC₅₀	6.2 nM Compound: 1; AZD-4547	Antiproliferative activity against human SNU16 cells expressing FGFR2 after 72 hrs Antiproliferative activity against human SNU16 cells expressing FGFR2 after 72 hrs	[PMID: 29775937]
SNU-16	IC₅₀	64 nM Compound: 8; AZD4547	Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay	[PMID: 33199155]

体外研究
(In Vitro)

Fexagratinib also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC₅₀ of 24 nM. In KG1a, Sum52-PE, MCF7, and KMS11 cell lines, Fexagratinib potently inhibits autophosphorylation of FGFR1, 2, and 3 tyrosine kinases (IC₅₀ values of 12, 2, and 40 nM, respectively) and displays weaker inhibition of FGFR4 cellular kinase activity (IC₅₀=142 nM). Significantly weaker inhibitory activity is observed versus cellular KDR and IGFR ligand-induced phosphorylation (IC₅₀ values of 258 and 828 nM, respectively), representing approximately 20- and 70-fold selectivity over cellular FGFR1. Besides, Fexagratinib potently inhibits FGFR phosphorylation and downstream signaling affected through FRS2, PLCγ, and MAPK at the cellular level^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Female SCID mice bearing KMS11 tumors are randomized and treated chronically with Fexagratinib at a range of well-tolerated doses. Oral Fexagratinib treatment results in dose-dependent tumor growth inhibition. Twice daily administration of Fexagratinib at 3 mg/kg gives statistically significant tumor growth inhibition of 53% (P<0.0005 by one-tailed t test) when compare with vehicle-treated controls, whereas doses of 12.5 mg/kg once daily and 6.25 mg/kg twice daily results in complete tumor stasis (P<0.0001). A further efficacy study in the KG1a model with 12.5 mg/kg once daily Fexagratinib results in 65% tumor growth inhibition (P=0.002)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

463.57

Formula

C₂₆H₃₃N₅O₃

CAS 号

1035270-39-3

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (269.65 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1572 mL	10.7859 mL	21.5717 mL
5 mM	0.4314 mL	2.1572 mL	4.3143 mL
10 mM	0.2157 mL	1.0786 mL	2.1572 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.39 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.49 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.49 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 1% CMC-Na/saline water
Solubility: 3.33 mg/mL (7.18 mM); 悬浊液; 超声助溶 (<60°C)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.85%

选择批次：

Data Sheet (628 KB) SDS (393 KB)

COA (289 KB) HNMR (289 KB) LCMS (91 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Gavine PR, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res, 2012, 72(8), 2045-2056. [Content Brief]

Cell Assay ^[1]	Cell lines are incubated with fixed concentrations of AZD4547 for 72 hours. For fluorescence-activated cell sorting (FACS), cells are fixed with 70% ethanol and then incubated with propidium iodide/RNase A labeling solution. Cell-cycle profiles are assessed with a FACSCalibur instrument and CellQuest analysis software. For apoptotic analysis, cells and media are gently harvested and centrifuged, followed by washing of cell pellets. Cells are then processed for FITC staining and propidium iodide uptake. The proportion of cells staining positive for Annexin V are then assessed with a FACSCalibur instrument and quadrant sorting is done by CellQuest analysis software^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Swiss derived nude (nu/nu) and severe combined immunodeficient mice (SCID) are used. Tumor xenografts are established by s.c. injection into the left flank with 0.1 mL tumor cells (1×10⁶ for LoVo, 1×10⁷ for HCT-15, and 1×10⁷ for Calu-6) or 0.2 mL (2×10⁷ for KMS11 and KG1a) mixed 1:1 with Matrigel, with the exception of LoVo and HCT-15, which do not include Matrigel. Mice are randomized into control and treatment groups (AZD4547, 1.5-50 mg/kg, once daily or twice daily by oral gavage) when tumors reach the determined size of more than 0.2 cm³. Tumor volume (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. Tumor volume is calculated. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Gavine PR, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res, 2012, 72(8), 2045-2056. [Content Brief]

Fexagratinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1572 mL	10.7859 mL	21.5717 mL	53.9293 mL
	5 mM	0.4314 mL	2.1572 mL	4.3143 mL	10.7859 mL
	10 mM	0.2157 mL	1.0786 mL	2.1572 mL	5.3929 mL
	15 mM	0.1438 mL	0.7191 mL	1.4381 mL	3.5953 mL
	20 mM	0.1079 mL	0.5393 mL	1.0786 mL	2.6965 mL
	25 mM	0.0863 mL	0.4314 mL	0.8629 mL	2.1572 mL
	30 mM	0.0719 mL	0.3595 mL	0.7191 mL	1.7976 mL
	40 mM	0.0539 mL	0.2696 mL	0.5393 mL	1.3482 mL
	50 mM	0.0431 mL	0.2157 mL	0.4314 mL	1.0786 mL
	60 mM	0.0360 mL	0.1798 mL	0.3595 mL	0.8988 mL
	80 mM	0.0270 mL	0.1348 mL	0.2696 mL	0.6741 mL
	100 mM	0.0216 mL	0.1079 mL	0.2157 mL	0.5393 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fexagratinib1035270-39-3AZD4547 ADSK091AZD 4547AZD-4547ADSK091ADSK 091ADSK-091FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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Fexagratinib (Synonyms: AZD4547; ADSK091)

Customer Review

Other Forms of Fexagratinib:

Fexagratinib 相关抗体

MCE 顾客使用本产品发表的 24 篇科研文献

Fexagratinib 相关产品

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生物活性

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