AZD4547

目录号：S2801

Molecular Weight(MW): 463.57

AZD4547是一种新型选择性的FGFR抑制剂，靶向作用于FGFR1/2/3，在无细胞试验中IC50为0.2 nM/2.5 nM/1.8 nM，对FGFR4， VEGFR2(KDR)具有微弱的作用活性，对IGFR， CDK2和p38几乎没有作用活性。Phase 2/3。

规格

价格

库存

购买数量

10mM (in 1mL DMSO)	RMB 1801.43	现货
5mg	RMB 901.31	现货
10mg	RMB 1395.39	现货
50mg	RMB 4661.52	现货
100mg	RMB 7125.05	现货
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客户购买Selleck的此次产品后发表的文献21篇：

客户使用该产品的6个实验数据：

Ependymoma cells and neural stem cell line 1 (NSC1) controls treated with or AZD4547 for 72 h and assessed using an Alamar Blue stain. Error bars show s.d. Experiment performed as six technical replicates and replicated in biological triplicates.

Nature, 2018, 553(7686):101-105. AZD4547 purchased from Selleck.

A-431 and ACHN cells that are partially sensitive to the EGFR inhibitor gefitinib were treated with gefitinib, the FGFR inhibitor AZD-4547, or a combination of both. Error bars depict SEM of three experiments. Cell viability and proliferation assays showed that the combination of the drugs was more effective than single compounds.

Science, 2017, doi: 10.1126/science.aan4368. AZD4547 purchased from Selleck.
Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 mmol/L BGJ398 assessed by immunoblotting.

Clin Cancer Res, 2017, 23(18):5527-5536. AZD4547 purchased from Selleck.

(b) Representative pictures of Vim expression in four groups. Bars=20 μm. (c) A box plot graph showing the quantitative evaluation of Vim staining intensity. A plot of a box plot with whiskers extending from the 5th to the 95th percentile of all the score data was used. (d) Representative pictures of Sirius red staining in tumor samples from 32 nude mice. Sirius red staining showed the increased collagen fiber in TGF +AZD group. Bars=100 μm. Percentage of positive area to total area is quantified.

Oncogene, 2017, 36(27):3831-3841. AZD4547 purchased from Selleck.
FCM evaluating lung CD11b+/Gr1+ myeloid cells isolated from 4T1 tumor-bearing mice after 20 days of treatment with AZD4547 or control. Statistical significance was assessed by unpaired t test.

Cell Physiol Biochem 2014 33(3), 633-45. AZD4547 purchased from Selleck.

Treatment of human CECs with of IL-1β (*, P < 0.01) and FGF2 (+, P < 0.01) resulted in enhanced cell migration as measured in a scratch-induced directional migration assay. Cotreatment with AZD4547 (AZD), an antagonist against FGF receptors 1 to 3, abolished the FGF2-enhanced (++, P < 0.01) but not the IL-1β-enhanced (P > 0.05) migration in human CECs. One-way ANOVA: F_{(4, 80)}= 512, P < 0.00001, n =17 per sample. Tukey's post hoc test, HSD_{[0.05]_{= 10.9; HSD_{[0.01]_{= 13.1.}}}}

Mol Cell Biol 2014 34(18), 3535-45. AZD4547 purchased from Selleck.

产品安全说明书

FGFR抑制剂选择性比较

生物活性

产品描述

特性

AZD4547高选择性作用于 FGFR1-3，比作用于FGFR4选择性高。AZD4547有效作用于野生型和突变型FGFR酪氨酸激酶活性。

靶点

FGFR1 ^[1] (Cell-free assay)	FGFR3 ^[1] (Cell-free assay)	FGFR2 ^[1] (Cell-free assay)	KDR ^[1] (Cell-free assay)
0.2 nM	1.8 nM	2.5 nM	24 nM

体外研究

与 FGFR1-3相比, AZD4547作用于FGFR4，活性微弱，IC50为165 nM。AZD4547 只抑制重组 VEGFR2 (KDR) 激酶活性， IC50为 24 nM,在体外选择性作用于一组多种代表性的人类激酶。0.1 μM AZD4547 作用于一系列重组激酶，包括 ALK, CHK1, EGFR, MAPK1, MEK1, p70S6K, PDGFR, PKB, Src, Tie2,和 PI3K，没有作用活性。相应地,在细胞磷酸化实验中，可观察到AZD4547 作用于FGFR1-3的选择性比作用于 FGFR4, IGFR, 和 KDR高。AZD4547在体外,只有作用于表达去调控FGFRs 如KG1a, Sum52-PE,和KMS11的肿瘤细胞，具有有效抗增殖活性，IC50 为18-281 nM,而对MCF7 及100 种以上其他肿瘤细胞无活性。AZD4547 处理人类肿瘤细胞，有效抑制FGFR 和 MAPK 磷酸化,这种作用存在剂量依赖性。AZD4547 也有效抑制FRS2 和 PLCγ磷酸化,及下游FGFR信号。另外, AZD4547作用于乳腺细胞系，MCF7和Sum52-PE 而不是KG1a和 KMS11细胞，影响AKT磷酸化。AZD4547处理Sum52-PE 和 KMS11细胞，显著诱导凋亡,作用于KG1a细胞，显著提高细胞周期在G1期停滞而不是凋亡, 而作用于MCF7细胞，对细胞周期分布和凋亡都没有作用效果。^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
SNU449	MnnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NX7UUmZPPzJiaB?=	MUnJR\|UxRTBwMEiyJO69VQ>?	MoDaNlY{PTF\|MkC=
SK-HEP-1	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M2nhRlczKGh?	Ml3vTWM2OD1yLkC4OEDPxE1?	NH3o[5EzPjN3MUOyNC=>
SNU475	NF3DfoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVjHd5lwPzJiaB?=	NFKyVmZKSzVyPUWuOEDPxE1?	MVqyOlM2OTN{MB?=
Hep3B	NVXMeFhiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		Mne1O\|IhcA>?	MYLJR\|UxRTZwNEOg{txO	Mk\KNlY{PTF\|MkC=
PLC/PRF5	MkD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIi3Z5E4OiCq	Mn7iTWM2OD14LkW1JO69VQ>?	M4XXV\|I3OzVzM{Kw
Hur7	M2PmVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NH76Wo44OiCq	NVPFTpF2UUN3ME23MlI2KM7:TR?=	NVXaTZVbOjZ\|NUGzNlA>
HepG2	NGfsUI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NHTvcZg4OiCq	NWHEOZRjUUN3ME24Mlc{KM7:TR?=	Ml3tNlY{PTF\|MkC=
SNU449	M17FVmNtd26xZ3XubYMh[XO\|YYm=	MX2xJOK2VQ>?	NXzNVXI{OjRiaB?=	Mke5[IVkemWjc3XzJINwdG:weTDmc5Ju[XSrb36gd4lodmmoaXPhcpRtgQ>?	MXKyOlM2OTN{MB?=
SK-HEP-1	NH;RboZEdG:wb3flcolkKGG\|c3H5	NXrMb4xlOSEEtV2=	MYWyOEBp	NHfn[YRl\WO{ZXHz[ZMh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7	NUfnR4FDOjZ\|NUGzNlA>
SNU449	NGLWbFhHfW6ldHnvckBCe3OjeR?=	M1jOeVAuOiEQvF2=	M3PUWlQ5KGh?	M13Pe4NifXOnczDhJIRm[3KnYYPlJI9nKE[UU{NvwKxCU1RuIHHu[EBGWkticHjvd5Bpd3K7bHH0bY9v	NFLvb5AzPjN3MUOyNC=>
SK-HEP-1	NY\6bVV[TnWwY4Tpc44hSXO\|YYm=	MonSNE0zKM7:TR?=	M{PwT\|Q5KGh?	NH;LUFdk[XW\|ZYOgZUBl\WO{ZXHz[UBw\iCIUmOy89yNSUuWLDDhcoQhTVKNIIDoc5NxcG:{eXzheIlwdg>?	MWqyOlM2OTN{MB?=
BaF3 FLT3-TEL	NXLLNZR[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NVXNeYQ{T0l3ME20MlYhyrFiMD61O\|ch\|ryP	M1rFSlI3Ojl2N{Sx
BaF3 RET-TEL	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MknrS2k2OD1yLkO5JOKyKDBwMES4JO69VQ>?	NIfGO4UzPjJ7NEe0NS=>
BaF3 Parental	M33mNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M1O2dGdKPTExubWxNEDPxE1?	MUSyOlI6PDd2MR?=
MOLM14 FLT3/ITD	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MUXHTVUxRTBwNEi0JOKyKDBwMUW3JO69VQ>?	MWKyOlI6PDd2MR?=
MV4-11 FLT3/ITD	NUXRd4hzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M4X6b2dKPTB;MD60OVkhyrFiMD6wOFYh\|ryP	MUeyOlI6PDd2MR?=
TT RET C634W	NGW1eYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MVrHTVUxRTJwOTFCtUAxNjlyNDFOwG0>	M17uXlI3Ojl2N{Sx
AN3-CA FGFR2 N550K, K310R	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NEjv[llIUTVyPUCuNFMyKMLzIECuNFI{KM7:TR?=	M{TFWVI3Ojl2N{Sx
MFE296 FGFR2 N550K	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NITCNZJIUTVyPUCuO\|MxKMLzIECuNFU4KM7:TR?=	M{HDV\|I3Ojl2N{Sx
MFE280 FGFR2 S252W	NFrYUJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M{PwXGdKPTB;MD6yNVghyrFiMD6wO\|Mh\|ryP	MkPmNlYzQTR5NEG=
Ishikawa FGFF2 over exp.	NFPENoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MnzYS2k2OD12LkWgxtEhOS53MTFOwG0>	NYjZb4tNOjZ{OUS3OFE>
HEC1A Normal FGFR2	NWLoPYoyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NVzw[GhMT0l3MP-5qVExKM7:TR?=	NHPSbI0zPjJ7NEe0NS=>
A549	NIPLcYpE\WyuII\pZYJqdGm2eTDBd5NigQ>?	NWPnZ49qOC5zL{Gg{txO	MmDYOFghcA>?	Mmr3[Y5p[W6lZYOgSZJtd3SrbnniJIlv\HWlZXSgeoli[mmuaYT5JIxwe3N?	MU[yOlA2OzB{MB?=
SGC-7901	MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVH4PHJiOSCwTT2xNEDPxE1?	MVW3NkBp	M3rCU2lEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	NXf0e4NoOjV3N{[5NVU>
HGC-27	M2\EeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXTFRmZ6OSCwTT2xNEDPxE1?	NV7WVJNIPzJiaB?=	NWH5SoNTUUN3MDDv[kA2NTFyIN88UUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=	M4S3SVI2PTd4OUG1
MKN-28	Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1n0RVEhdk1vMUCg{txO	NV70[IFIPzJiaB?=	MXnJR\|UxKG:oIEWtNVAh\|ryPLDDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6	NU\iNoZVOjV3N{[5NVU>
NCI-N87	NE[xN3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NI\WVXoyKG6PLUGwJO69VQ>?	MmnkO\|IhcA>?	M4f3SmlEPTBib3[gOU0yOCEQvF2sJIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?	MVmyOVU4PjlzNR?=
KATOIII	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkezNUBvVS1zMDFOwG0>	M1rNPFczKGh?	NEXKTWJKSzVyIH;mJFExNTFyMDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=	M4C4b\|I2PTd4OUG1
SNU-16	NV\C[ms{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MX[xJI5ONTFyIN88US=>	M2LJcVczKGh?	MVXJR\|UxKG:oIEGwMVExOCCwTTygbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>?	NVviO3JUOjV3N{[5NVU>
4T1	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MX;JR\|UxRTBwNkVCtVAvOTFizszN	NYH3XVVIOjR4NEK4PVM>
MDA-MB-468	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MYnJR\|UxRTRwOdMxNE45PSEQvF2=	NITqb4IzPDZ2Mki5Ny=>
HCT116	M1nIVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MVjJR\|UxRTF3LkpCtVEvQDJizszN	MoH6NlQ3PDJ6OUO=
SW620	M1j0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MlXtTWM2OO,:nkKwJO69VQ>?	MmSxNlQ3PDJ6OUO=
MDA-MB-231	NEGwZ45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NVTxSYF7UUN3MP-8olIxKM7:TR?=	MkH6NlQ3PDJ6OUO=
CT26	Mo[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NVXYd5lvUUN3MP-8olIxKM7:TR?=	NXK5N4RHOjR4NEK4PVM>
SW480	MlLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M3\XRWlEPTExvK6yNEDPxE1?	NWTV[\|ZXOjR4NEK4PVM>
4T1	NHvLeZNCeG:ydH;zbZMhSXO\|YYm=	M{i2TlEvOjVvMkCg{txO	M{OxNFI1KGh?	M2PqdYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm=	M4T0ZVI1PjR{OEmz
KG1a	M2jVRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M1z3cGlEPTB;MD6wNVgh\|ryP	M{f4XVIzOzZ7OUK4
Sum52-PE	M2r6Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NHjXdoxKSzVyPUCuNFQyKM7:TR?=	NITuS5EzOjN4OUmyPC=>
KMS11	NFvEeWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MVPJR\|UxRTBwMkixJO69VQ>?	M3zQUVIzOzZ7OUK4
MCF7	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFPjOnBKSzVyPkOwJO69VQ>?	NFzSWnkzOjN4OUmyPC=>

... Click to View More Cell Line Experimental Data

体内研究

AZD4547按3 mg/kg剂量口服处理携带KMS11肿瘤的小鼠，每天两次，与空白对照组相比，显著抑制53%肿瘤生长，AZD4547 按 12.5 mg/kg剂量每天处理一次，或按 6.25 mg/kg剂量每天处理两次，则完全抑制肿瘤，这与p-FGFR3的药效学调节剂量正相关，且降低 KMS11肿瘤细胞增殖。而且, AZD4547按 12.5 mg/kg剂量口服处理给药FGFR1融合KG1a 移植瘤模型，每天一次，抑制65% 肿瘤生长。在有效剂量水平，AZD4547不表现出抗血管生成的效果。AZD4547 对血压没有显著作用效果，因此在体内缺乏抗-KDR 活性。相应地, AZD4547按6.25 mg/kg剂量口服处理对Cediranib敏感的移植瘤模型，包括 Calu-6, HCT-15 和 LoVo，每天两次，没有作用活性。^[1]

激酶实验：^[1]	+ 展开 AZD4547 激酶活性: 使用浓度等于或低于相对K_m 的ATP，测定AZD4547抑制 FGFR1-3的人类重组激酶活性的效果。
细胞实验：^[1]	+ 展开 Cell lines: KG1a, Sum52-PE, KMS11, 和MCF7 Concentrations: 溶于DMSO,终浓度为 ~1 μM Incubation Time: 72 小时 Method: 使用多种浓度AZD4547处理细胞72小时。通过 MTS 增殖实验获得抗增殖的IC50值。荧光激活细胞分选(FACS)中,细胞与70%乙醇混合，然后与碘化丙啶/RNase A标记溶液温育。使用 FACSCalibur 仪器和CellQuest分析软件测定细胞周期谱。为了分析凋亡，轻轻收集细胞和培养基，离心，然后冲洗细胞颗粒。细胞进行Annexin膜联蛋白 V-异硫氰酸荧光素(FITC)染色和碘化丙啶吸收。使用FACSCalibur仪器测定膜联蛋白 V染色阳性细胞比例，使用CellQuest分析软件进行象限分类。 (Only for Reference)
动物实验：^[1]	+ 展开 Animal Models: 皮下注射LoVo, HCT-15, Calu-6, KMS11 或 KG1a的雌性Swiss衍生裸鼠和SCID小鼠 Formulation: 在去离子水的 1% (v/v)Tween-80溶液中配制 Dosages: 1.5-50 mg/kg Administration: 口服饲喂，每天一次或两次 (Only for Reference)

参考文献

[1] Gavine PR, et al. Cancer Res, 2012, 72(8), 2045-2056.

溶解度 (25°C)

体外	DMSO	92 mg/mL (198.45 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 4% DMSO+30% PEG 300+5% Tween 80+ddH2O	5mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download AZD4547 SDF

分子量	463.57
化学式	C₂₆H₃₃N₅O₃
CAS号	1035270-39-3
稳定性	3 years -20°C powder
稳定性	2 years -80°C in solvent
别名	N/A

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2018-11-16)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02546661	Recruiting	Muscle Invasive Bladder Cancer	AstraZeneca	October 3 2016	Phase 1
NCT02824133	Suspended	Recurrent IDHwt Gliomas With FGFR3-TACC3 Fusion\|Recurrent IDHwt Gliomas With FGFR1-TACC1 Fusion	Assistance Publique - Hôpitaux de Paris	September 2015	Phase 1\|Phase 2
NCT02465060	Recruiting	Advanced Malignant Solid Neoplasm\|Bladder Carcinoma\|Breast Carcinoma\|Cervical Carcinoma\|Colon Carcinoma\|Colorectal Carcinoma\|Endometrial Carcinoma\|Esophageal Carcinoma\|Gastric Carcinoma\|Glioma\|Head and Neck Carcinoma\|Kidney Carcinoma\|Liver and Intrahepatic Bile Duct Carcinoma\|Lung Carcinoma\|Lymphoma\|Malignant Uterine Neoplasm\|Melanoma\|Ovarian Carcinoma\|Pancreatic Carcinoma\|Plasma Cell Myeloma\|Prostate Carcinoma\|Rectal Carcinoma\|Recurrent Bladder Carcinoma\|Recurrent Breast Carcinoma\|Recurrent Cervical Carcinoma\|Recurrent Colon Carcinoma\|Recurrent Colorectal Carcinoma\|Recurrent Esophageal Carcinoma\|Recurrent Gastric Carcinoma\|Recurrent Glioma\|Recurrent Head and Neck Carcinoma\|Recurrent Liver Carcinoma\|Recurrent Lung Carcinoma\|Recurrent Lymphoma\|Recurrent Malignant Solid Neoplasm\|Recurrent Melanoma\|Recurrent Ovarian Carcinoma\|Recurrent Pancreatic Carcinoma\|Recurrent Plasma Cell Myeloma\|Recurrent Prostate Carcinoma\|Recurrent Rectal Carcinoma\|Recurrent Skin Carcinoma\|Recurrent Thyroid Gland Carcinoma\|Recurrent Uterine Corpus Carcinoma\|Refractory Lymphoma\|Refractory Malignant Solid Neoplasm\|Refractory Plasma Cell Myeloma\|Skin Carcinoma\|Thyroid Gland Carcinoma\|Uterine Corpus Cancer	National Cancer Institute (NCI)	August 12 2015	Phase 2
NCT02664935	Recruiting	Non-Small Cell Lung Cancer\|Carcinoma Squamous Cell\|Adenocarcinoma	University of Birmingham\|Cancer Research UK\|AstraZeneca\|Pfizer\|Experimental Cancer Medicine Centre Network\|Mirati Therapeutics Inc.	May 2015	Phase 2
NCT02965378	Active not recruiting	FGFR1 Gene Amplification\|FGFR1 Gene Mutation\|FGFR2 Gene Amplification\|FGFR2 Gene Mutation\|FGFR3 Gene Amplification\|FGFR3 Gene Mutation\|Recurrent Squamous Cell Lung Carcinoma\|Stage IV Squamous Cell Lung Carcinoma AJCC v7	Southwest Oncology Group\|National Cancer Institute (NCI)	June 16 2014	Phase 2\|Phase 3
NCT02154490	Recruiting	Recurrent Squamous Cell Lung Carcinoma\|Stage IV Squamous Cell Lung Carcinoma AJCC v7	Southwest Oncology Group\|National Cancer Institute (NCI)	June 16 2014	Phase 2\|Phase 3

技术支持

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操作手册

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FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

选择性强的FGFR抑制剂

PD173074 : FGFR1-selective, IC50=~25 nM.
FDA批准的FGFR抑制剂

Ponatinib (AP24534) : Approved by FDA for resistant or intolerant CML and Ph+ ALL.
最新的FGFR抑制剂

SSR128129E ^New : Orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
经典的FGFR抑制剂

Dovitinib (TKI-258, CHIR-258) : Multitargeted RTK inhibitor for class III (FLT3/c-Kit), class IV (FGFR1/3) and class V (VEGFR1-4) RTKs.

研究领域

产品类型

AZD4547

客户购买Selleck的此次产品后发表的文献21篇：

客户使用该产品的6个实验数据：

产品安全说明书

FGFR抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download AZD4547 SDF

计算器

摩尔浓度计算器

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2018-11-16)

技术支持

FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

相关FGFR产品