PD173074

For research use only. Not for use in humans.

Pfizer辉瑞授权目录号：S1264

CAS No. 219580-11-7

PD173074 是一种有效的FGFR1抑制剂，在无细胞试验中IC50约为25 nM，也能抑制VEGFR2，IC50为100-200 nM，作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。PD173074 可在胃癌细胞中抑制增殖并促进凋亡。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 802.11	现货
5mg	RMB 575.36	现货
50mg	RMB 3867.14	现货
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客户使用Selleck生产的PD173074发表文献96篇：

Cell Stem Cell, 2020, S1934-5909(20)30541-5

PubMed: 33271070 ( click the link to review the publication )

Cancer Cell, 2019, 35(3):504-518

PubMed: 30827889 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Nat Genet, 2015, 47(9):1003-10

PubMed: 26258846 ( click the link to review the publication )

Nat Methods, 2014, 11(8):855-60

PubMed: 24930130 ( click the link to review the publication )

Cancer Discov, 2013, 3(6):636-47

PubMed: 23558953 ( click the link to review the publication )

Science, 2011, 331(6019):912-6

PubMed: 21330545 ( click the link to review the publication )

Adv Sci (Weinh), 2021, 8(2):2002922

PubMed: 33511016 ( click the link to review the publication )

Nat Commun, 2021, 12(1):3017

PubMed: 34021145 ( click the link to review the publication )

EMBO J, 2021, e107182

PubMed: 34086370 ( click the link to review the publication )

Int J Mol Sci, 2021, 22(9)4720

PubMed: 33946884 ( click the link to review the publication )

Invest New Drugs, 2021, 10.1007/s10637-021-01061-1

PubMed: 33829354 ( click the link to review the publication )

J Exp Med, 2020, 3;217(8):e20191805

PubMed: 32434218 ( click the link to review the publication )

Leukemia, 2020, 14

PubMed: 32409689 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2020, 202008017

PubMed: 32989154 ( click the link to review the publication )

Redox Biol, 2020, 38:101780

PubMed: 33171331 ( click the link to review the publication )

Front Oncol, 2020, 10;10:331

PubMed: 32211337 ( click the link to review the publication )

Front Oncol, 2020, 10:584505

PubMed: 33425737 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(9)E3214

PubMed: 32370101 ( click the link to review the publication )

Front Pharmacol, 2020, 11:154

PubMed: 32184729 ( click the link to review the publication )

Neuroscience, 2020, 1;436:1-10

PubMed: 32278061 ( click the link to review the publication )

PLoS One, 2020, 15(6):e0234708

PubMed: 32555680 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(3)

PubMed: 32024006 ( click the link to review the publication )
NPJ Breast Cancer, 2020, 6:30

PubMed: 32715085 ( click the link to review the publication )

Stem Cell Res, 2020, 48:101951

PubMed: 32798915 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0713

PubMed: 31409615 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-18-2779

PubMed: 31515463 ( click the link to review the publication )

Cell Rep, 2019, 28(9):2331-2344

PubMed: 31461650 ( click the link to review the publication )

Elife, 2019, 8

PubMed: 30720426 ( click the link to review the publication )

Development, 2019, 146(14)

PubMed: 31320324 ( click the link to review the publication )

Cells, 2019, 8(3)

PubMed: 30866584 ( click the link to review the publication )

Exp Neurol, 2019, 317:34-50

PubMed: 30802446 ( click the link to review the publication )

Lab Invest, 2019, 10.1038/s41374-019-0256-3

PubMed: 31028279 ( click the link to review the publication )

Sci Rep, 2019, 9(1):7037

PubMed: 31065021 ( click the link to review the publication )

Respir Res, 2019, 20(1-:270

PubMed: 31791326 ( click the link to review the publication )

Cancer Res Treat, 2019, 51(3):951-962

PubMed: 30309221 ( click the link to review the publication )

ACS Comb Sci, 2019, 21(12):805-816

PubMed: 31689077 ( click the link to review the publication )

Oncotarget, 2019, 10(11):1171-1192

PubMed: 30838090 ( click the link to review the publication )

Stem Cell Reports, 2018, 10(4):1308-1323

PubMed: 29526737 ( click the link to review the publication )

Cell Physiol Biochem, 2018, 47(1):151-160

PubMed: 29763898 ( click the link to review the publication )

Osteoarthritis Cartilage, 2018, 26(12):1733-1743

PubMed: 30201491 ( click the link to review the publication )

Mol Oncol, 2018, 10.1002/1878-0261.12422

PubMed: 30537101 ( click the link to review the publication )

Cells, 2018, 7(12)

PubMed: 30544798 ( click the link to review the publication )

J Cell Sci, 2018, 131(18)

PubMed: 30154213 ( click the link to review the publication )

Int J Biol Sci, 2018, 14(10):1389-1398

PubMed: 30123084 ( click the link to review the publication )

Front Neurosci, 2018, 12:582

PubMed: 30210273 ( click the link to review the publication )

Cancer Biol Ther, 2018, 19(1):76-86

PubMed: 29257923 ( click the link to review the publication )
Dev Biol, 2018, 433(2):394-403

PubMed: 29291983 ( click the link to review the publication )

Dev Biol, 2018, 433(2):416-432

PubMed: 28760345 ( click the link to review the publication )

Biomed Pharmacother, 2018, 103:1516-1525

PubMed: 29864937 ( click the link to review the publication )

Nat Commun, 2017, 8;8:15617

PubMed: 28593995 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(4):962-973

PubMed: 27535980 ( click the link to review the publication )

Cell Syst, 2017,

PubMed: 28017544 ( click the link to review the publication )

ACS Appl Mater Interfaces, 2017, 9(45):39185-39196

PubMed: 29045789 ( click the link to review the publication )

Elife, 2017, 10.7554/eLife.25946

PubMed: 28598329 ( click the link to review the publication )

Sci Rep, 2017, 7:41986

PubMed: 28155881 ( click the link to review the publication )

Am J Physiol Endocrinol Metab, 2017, ajpendo.00328.2016

PubMed: 28174179 ( click the link to review the publication )

PLoS One, 2017, 12(2):e0171898

PubMed: 28207787 ( click the link to review the publication )

J Orthop Sci, 2017, 22(6):1112-1119

PubMed: 28877850 ( click the link to review the publication )

Oncotarget, 2017, 8(54):91841-91859

PubMed: 29190880 ( click the link to review the publication )

Tumour Biol, 2017, 39(7):1010428317712592

PubMed: 28718374 ( click the link to review the publication )

Stem Cell Reports, 2017, 8(1):84-94

PubMed: 28076758 ( click the link to review the publication )

Nat Commun, 2016, 7:13796

PubMed: 27982029 ( click the link to review the publication )

Cancer Res, 2016, 10.1158/0008-5472.CAN-16-0058

PubMed: 27231203 ( click the link to review the publication )

Cancer Res, 2016, 76(22):6471-6482

PubMed: 27671675 ( click the link to review the publication )

Biomaterials, 2016, 78:115-28

PubMed: 26691234 ( click the link to review the publication )

J Neurosci, 2016, 36(16):4534-48

PubMed: 27098696 ( click the link to review the publication )

Cell Oncol (Dordr), 2016, 39(3):229-42

PubMed: 26883759 ( click the link to review the publication )

Dev Biol, 2016, 415(2):228-241

PubMed: 26988119 ( click the link to review the publication )

Development, 2016, 143(23):4368-4380

PubMed: 27660325 ( click the link to review the publication )

Oncotarget, 2016,

PubMed: 27153554 ( click the link to review the publication )
Oncotarget, 2016, 7(31-:50161-50179

PubMed: 27367030 ( click the link to review the publication )

J Thorac Oncol, 2015, 10(12):1736-44

PubMed: 26473643 ( click the link to review the publication )

Cancer Res, 2015, 75(5):880-91

PubMed: 25432174 ( click the link to review the publication )

Mol Cancer Ther, 2015, 14(12):2831-9

PubMed: 26438159 ( click the link to review the publication )

Carcinogenesis, 2015, 36(1):32-40

PubMed: 25344834 ( click the link to review the publication )

Cancer Sci, 2015, 106(10):1278-87

PubMed: 26183471 ( click the link to review the publication )

Exp Cell Res, 2015, 332(2):223-35

PubMed: 25704758 ( click the link to review the publication )

Growth Factors, 2015, 33(5-6):356-65

PubMed: 26607681 ( click the link to review the publication )

Gut, 2014, 63(12):1932-42

PubMed: 24658599 ( click the link to review the publication )

Blood, 2014, 123(10):1516-24

PubMed: 24408322 ( click the link to review the publication )

Hepatology, 2014, 59(4):1427-34

PubMed: 24122810 ( click the link to review the publication )

Gastric Cancer, 2014, 10.1007/s10120-014-0444-1

PubMed: 25407459 ( click the link to review the publication )

Neoplasia, 2014, 16(8):644-55

PubMed: 25220592 ( click the link to review the publication )

J Cell Sci, 2014, 127(Pt 23):5079-92

PubMed: 25278553 ( click the link to review the publication )

J Cell Sci, 2014, 127(23):5079-92

PubMed: ( click the link to review the publication )

Breast Cancer Res Tr, 2014, 143(3):435-46

PubMed: 24398778 ( click the link to review the publication )

Cancer Biol Ther, 2014, 15(12):1613-21

PubMed: 25535896 ( click the link to review the publication )

PLoS One, 2014, 9(4):e95434

PubMed: 24752320 ( click the link to review the publication )

Mol Cancer Res, 2013, 11(12):1585-96

PubMed: 24092775 ( click the link to review the publication )

PLoS One, 2013, 8(2):e56735

PubMed: 23468877 ( click the link to review the publication )

Celon Pharma Inc, 2013, Paulina Grygielewicz

PubMed: ( click the link to review the publication )

PLoS Genet, 2012, 8(2):e1002500

PubMed: 22383889 ( click the link to review the publication )

Mol Cell Proteomics, 2012, 11(9):745-57

PubMed: 22700489 ( click the link to review the publication )

Clin Exp Metastasis, 2012, 30(4):507-20

PubMed: 23212305 ( click the link to review the publication )

产品安全说明书

FGFR抑制剂选择性比较

生物活性

产品描述

靶点

FGFR1 ^[1] (Cell-free assay)	VEGFR2 ^[1] (Cell-free assay)
~25 nM	100 nM-200 nM

体外研究

PD173074是FGFR1的ATP竞争性抑制剂， K_i约为40 nM。PD173074也是VEGFR2的有效抑制剂。相比FGFR1，PD173074弱抑制Src，INSR，EGFR，PDGFR，MEK和PKC的活性，IC 50值大1000倍以上。PD173074剂量依赖性地抑制FGFR1和VEGFR2的自身磷酸化，IC50 分别为1-5 nM和100-200 nM。^[1] PD173074以剂量依赖的方式抑制FGF-2促进的颗粒神经元存活，IC50是12 nM，活性是SU 5402的1,000倍以上。^[2] D173074特异性地抑制FGF-2-介导的少突胶质细胞（OL）谱系细胞的细胞增殖，分化和MAPK激活。^[3] 在多发性骨髓瘤（MM）细胞系中，PD173074对野生受体和FGFR3突变有活性。PD173074还以剂量依赖的方式有效地抑制FGFR3的自磷酸化，IC50约为5 nM。PD173074有力地降低了表达FGFR3的KMS11细胞和KMS18细胞的活力，IC50小于20 nM。aFGF刺激的MM细胞生长受PD173074抑制是和FGFR3的表达高度相关的。PD173074完全抑制由Y373C FGFR3介导而不是的Ras介导的NIH 3T3转化，这表明PD173074专门针对FGFR3基因介导的细胞转化和缺乏非特异性的细胞毒性作用。PD173074也诱导KMS11和KMS18细胞功能成熟。^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
NCI-H1581	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NWTZ[FFXUUN3ME2wMlAyOjJ3IN88US=>	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
KG-1	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NULtUpZpUUN3ME2wMlA2OTJ7IN88US=>	Mk\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
MFM-223	MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NXrhelRGUUN3ME2wMlIyPTd4IN88US=>	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
EoL-1-cell	Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NGjxeVJKSzVyPUCuN\|I6QDRizszN	NF\xXY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK\|5USU6JRWK8M4E,
ECC10	M3jSW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MVnJR\|UxRTBwM{O4PVgh\|ryP	M3\2OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
H-EMC-SS	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFL0do1KSzVyPUCuN\|Q4OTVizszN	M12zNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
AN3-CA	NI\FeJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NY\QUWRCUUN3ME2wMlQxOTN\|IN88US=>	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
HuO-3N1	NFz1eoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NHmxZpNKSzVyPUCuOVQ3PTNizszN	MkXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
RT-112	NWr5SVVZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MYjJR\|UxRTBwNUS3NFEh\|ryP	MkjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
NEC8	NYfwOYFYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NE\uR4JKSzVyPUCuOVYzQDlizszN	NIS3WWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK\|5USU6JRWK8M4E,
D-263MG	NX\aeJQxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NWfybHE4UUN3ME2wMlcyOTV7IN88US=>	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
SW962	NYTXOlJST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MljpTWM2OD1yLke4PVg5KM7:TR?=	MlvGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
BV-173	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Mnn2TWM2OD1yLki0OlI{KM7:TR?=	M1PYTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
MFE-280	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MYPJR\|UxRTBwOEW4O\|Ih\|ryP	NIPTdG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK\|5USU6JRWK8M4E,
HuH-7	M3rhb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NIXHZmpKSzVyPUGuNlQ1PjRizszN	M2rSbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
RS4-11	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MnfwTWM2OD1zLkOzPFg3KM7:TR?=	NELKNYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK\|5USU6JRWK8M4E,
DMS-114	MnPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NV;N[o8{UUN3ME2xMlM3PzN5IN88US=>	M3\Ke\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
MSTO-211H	NWntW5FNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			Mnq4TWM2OD1zLkS3N\|c5KM7:TR?=	M1rHbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
DU-145	MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NGrTdlVKSzVyPUGuOVgzOTdizszN	NFXhTXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK\|5USU6JRWK8M4E,
A172	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFTSPWlKSzVyPUGuO\|A{PTVizszN	M3e5UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTV6ND:nQnNCVkeHUkyvZV4>
SBC-1	M{TNfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NEH1TmhKSzVyPUKuNFk1KM7:TR?=	NV3mOGN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
H9	NXjsSopxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NX22[INDUUN3ME2yMlE1OzB4IN88US=>	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
NCI-SNU-1	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Mo\UTWM2OD1{LkG4N\|k1KM7:TR?=	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk2QDRxJ{7TRW5ITVJ:L3G+
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NCI-H1437	NEfmS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NYW3NnpNUUN3ME20Ok4{OjFizszN	MmLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6PTh2Lze+V2FPT0WUPD;hQi=>
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OVCAR-8	NFHYOHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MVrJR\|UxRTR5Lk[4N{DPxE1?	NHfybGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl3OESvK\|5USU6JRWK8M4E,
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NCI-N87	MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NYrhUnEzUUN3ME20PE4zQTlzIN88US=>	NWrQbGdPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7NUi0M{c,W0GQR1XSQE9iRg>?
SUM52	M4OwOWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MnHpOUBl[Xm\|	MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE[JRmKyMYFueGyrZnnl[EBUXU13MjDj[YxteyCjZoTldkA2KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5yMUKzJO69VS5?	M4DFO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUKxNVU3Lz5{OEWyNVE2PjxxYU6=
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insect cells	NHnp[pdHfW6ldHnvckBie3OjeR?=		M1vw[FExKG2rboO=	NGPlT4RKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKGi3bXHuJGZITlJzIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCrboPlZ5Qh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiW3fhcY1iNTN{UG3BWHAh[W[2ZYKgNVAhdWmwczDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pIHLhd4VlKHKjZHnvZYN1cX[nIH\pcJRmeiCkaX7kbY5oKGG\|c3H5MEBKSzVyIE2gNE4xOjF3IN88UU4>	Ml\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUSzOlIoRjJ5OUG0N\|YzRC:jPh?=
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NCI-H520	NV62WmxXSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MUe3JIRigXN?	M4XUUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRlfGVlEu[W2ybHnmbYVlKE6FST3IOVIxKGOnbHzzJIFnfGW{IEeg[IF6eyCkeTDTVmIh[XO\|YYmsJGlEPTBiPTCwMlI5OSEQvF2u	NVvneWJSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1NlEyPTZpPkK4OVIyOTV4PD;hQi=>
HUVEC	MVfGeY5kfGmxbjDhd5NigQ>?	MVOxNEBvVQ>?	MnH1NVQhcHK\|	NGm0VIZKdmirYnn0bY9vKG:oIF\HSnIudWWmaXH0[YQh[W6paX;n[Y5me2m\|IHnuJIh2dWGwIFjVWmVEKGOnbHzzJIF{e2W\|c3XkJIF{KGSnY4LlZZNmKGmwIHPhdIltdGG{eTD0eYJmKHOycn;1eIlv\yCjdDCxNEBvVSCjZoTldkAyPCCqcoO=	MoTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ2N{SzPFcoRjF4NEe0N\|g4RC:jPh?=
HUVEC	M4\KNWZ2dmO2aX;uJIF{e2G7	Mo\qNVAxKG6P	NEO0RZQyPCCqcoO=	M{e1WWlvcGmkaYTpc44hd2ZiRlfGVk1u\WSrYYTl[EBidmerb3flcoV{cXNiaX6gbJVu[W5iSGXWSWMh[2WubIOgZZN{\XO\|ZXSgZZMh\GWlcnXhd4UhcW5iY3HwbYxt[XK7IIT1ZoUhe3C{b4X0bY5oKGG2IEGwNEBvVSCjZoTldkAyPCCqcoO=	NHL1c3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkS3OFM5Pyd-MU[0O\|Q{QDd:L3G+
SJ-GBM2	NWDDTpA6eUiWUzDhd5NigQ>?			NXvwRWFVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM>	NYr3cY92RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673	NHn4NHRyUFSVIHHzd4F6			NV2xS3NweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFG2O\|Mh[2WubIO=	NWrldVhZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	MkTYdWhVWyCjc4PhfS=>			NUfwcWpkeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	M1[3b\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37	M1XQ[5FJXFNiYYPzZZk>			NIjr[oVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN\|ch[2WubIO=	M3nkU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH	MU\xTHRUKGG\|c3H5			NGrqXXVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=>	NVe5fYJvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5	NH3WUWFyUFSVIHHzd4F6			NVLrU41seUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-12	MVfxTHRUKGG\|c3H5			MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh18	NYrUbItCeUiWUzDhd5NigQ>?			NWnJd3FqeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO=	MlTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
OHS-50	MojvdWhVWyCjc4PhfS=>			NHryO\|VyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz	NFjPcWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
RD	NFTKTXZyUFSVIHHzd4F6			MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM>	NX;qfWVRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
fibroblast cells	MVjxTHRUKGG\|c3H5			M4P5bZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy\|	NGnHeHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	NUPMWpFPeUiWUzDhd5NigQ>?			M3Sx[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy\|	MoLMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pFGFR2 / FGFR2 ; PubMed: 24968263 PLoS One PD173074 and MK2461 inhibit FGFR2 phosphorylation. Cells were treated for 1 hour with a titration of PD173074 as described in Materials and methods. Lysates were prepared and 50 ug protein was subjected to SDS-PAGE and western blotting with phospho Y653/654 FGFR and MAB6841 total FGFR2 antibody. p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1; PubMed: 24968263 PLoS One Time course of inhibition for multiple signaling proteins. NCI-H716 cells were treated with 100 nM PD173074 for the indicated times and signaling pathways were analyzed by SDS PAGE and western blotting. 100 nM PD173074 was selected because this amount caused full inhibition of pERK at the 2 hour time point. “p” indicates phosphoprotein, and the phosphorylation sites are listed in Methods. Terminology on the right side of figure groups proteins according to the time at which inhibition or protein loss occurs.	24968263
Growth inhibition assay	Cell viability; PubMed: 24968263 PLoS One B. PD173074 and MK2461 inhibit NCI-H716 cell growth. Cell lines were plated at 4000 cells/well and incubated overnight. NCI-H716 cells were treated with a titration of PD173074 as described in Materials and Methods. Cell growth was measured with Vialight reagent, and growth was presented relative to untreated cells. C. PD173074 and MK2461 selectively inhibit growth of NCI-H716 cells. Colon cancer cell lines listed were plated at 4000 cells/well and 24 hours later were treated with a titration of compounds. 4 days later cell growth was measured with vialight and IC50s were calculated from graph pad prism.	24968263

体内研究

PD173074在1 mg/kg/day或2 mg/ka/day对小鼠给药可以剂量依赖性的方式有效阻止由FGF或VEGF诱导的血管生成，并没有明显的毒性。^[1] PD173074抑制FGFR3突变体转染的NIH 3T3细胞在裸鼠体内生长。在KMS11异种移植瘤模型中，PD173074抑制FGFR3导致肿瘤生长延缓，小鼠的存活率提高。^[4] 在H-510异种移植体中，PD173074阻断肿瘤生长和cisplatin相似，与对照假治疗的动物相比增加中位生存期。在H-69异种移植体中，PD173074在50％小鼠中的诱导作用长于6个月。这些效应是和切除肿瘤中增加的细胞凋亡相关的，而非破坏肿瘤血管。^[5]

激酶实验：^[1]	- 合并体外激酶抑制试验: 检测是使用全长FGFR-1激酶在100微升含25 mM HEPES缓冲液（pH7.4），150 mM氯化钠，10 mM MnCl_{2，0.2 mM的原钒酸钠，750 μg/mL谷氨酸和酪氨酸（4:1）的无规共聚物，各种浓度的PD173074，和60至75 ng酶中进行的。该反应通过加入[γ-³²P]ATP（含有0.4 μCi of [γ-³²P]ATP的5 μM ATP）起始，样品在25°C孵育10分钟。反应通过加入30％三氯乙酸和材料的沉淀到玻璃纤维滤垫上终止。过滤器用15％三氯乙酸洗涤三次，掺入[³²P]到谷氨酸酪氨酸聚合物衬底是通过计算保留在过滤器上的放射性来确定，通过WALLAC1250 betaplate阅读器读取。非特异性的活性被定义为温育不含酶的样品保留在过滤器上放射性。特异活性被确定为总活性（酶加缓冲液）减去非特异性活性。PD173074抑制FGFR-1的酶活性的IC50浓度用图解法测定。}
细胞实验：^[4]	- 合并 Cell lines: KMS11和 KMS18 Concentrations: 溶解在DMSO中至终浓度~100 nM Incubation Time: 48小时 Method: 在aFGF/肝素的存在下，细胞在PD173074浓度梯度中孵育48小时。活细胞的百分比由MTT法检测。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 诱导角膜新生血管的瑞士韦伯斯特小鼠 Dosages: 约2 mg/kg/day Administration: 腹腔注射 (Only for Reference)

参考文献

- 合并

溶解度 (25°C)

体外	DMSO	100 mg/mL (190.95 mM)
	Ethanol	100 mg/mL (190.95 mM)
	Water	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)： 5% DMSO+corn oil	15mg/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 PD173074 SDF

分子量	523.67
化学式	C₂₈H₄₁N₇O₃
CAS号	219580-11-7
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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 (mg) = 浓度 (mM) x 体积 (mL) 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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
What is the half-life of PD173074(S1264) in vivo?
回答：
According to literature research, PD173074 is given twice daily because it has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.

FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

泛FGFR抑制剂

BGJ398 (NVP-BGJ398) : FGFR1/2/3-selective, IC50=0.9 nM/1.4 nM/1 nM.
活性最高的FGFR抑制剂

AZD4547 : FGFR1, IC50=0.2 nM; FGFR2, IC50=2.5 nM; FGFR3, IC50=1.8 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.

研究领域

产品类型

定制您的化合物库

PD173074

客户使用Selleck生产的PD173074发表文献96篇：

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 PD173074 SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) 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

技术支持

常见问题及建议解决方法

FGFR Signaling Pathway Map

FGFR Inhibitors with Unique Features

相关FGFR产品