PDGFR

Inhibitory Selectivity

Catalog No.	Inhibitor Name	PDGFR	PDGFRα	PDGFRβ	Other
A10001	Sorafenib Tosylate	**		**	Raf-1,VEGFR2/Flk1,B-Raf
A10468	Imatinib Mesylate				c-Kit,v-Abl
A10880	Sunitinib Malate			****	FLT3,Kit,VEGFR2
A10080	Ponatinib		****		Abl,VEGFR2,FGFR1
A10103	Axitinib		***	****	VEGFR1/FLT1,VEGFR2/Flk1,VEGFR3
A10259	Imatinib	**			c-Kit,v-Abl
A10137	Nintedanib		**	**	VEGFR3,VEGFR2,LCK
A10699	Pazopanib HCl	**			VEGFR1,VEGFR2,VEGFR3
A11411	Dovitinib		*	***	FLT3,c-Kit,FGFR1
A10025	Linifanib			**	VEGFR1/FLT1,CSF-1R,FLT3
A11052	Crenolanib		****	****
A10558	Masitinib		*	*	Kit,Lyn B,Abl1
A10101	Tivozanib		***	**	VEGFR2,VEGFR3,EphB2
A10610	Amuvatinib		***		c-Kit (D816H),FLT3 (D835Y)
A10608	Motesanib Diphosphate	**			VEGFR1,VEGFR2,VEGFR3
A10953	Orantinib			***	FGFR1,Flk1
A11350	CP-673451		***	****	c-Kit,VEGFR2,VEGFR1
A10502	Ki8751		**		VEGFR2,c-Kit,FGFR2
A10903	Telatinib		***		c-Kit,VEGFR3,VEGFR2
A11207	PP121	****			Hck,VEGFR,mTOR
A11518	Pazopanib	**			VEGFR1,VEGFR2,VEGFR3
A10504	KRN 633		*	*	VEGFR3,VEGFR2,VEGFR1
A10198	Dovitinib Dilactic Acid		*	***	FLT3,c-Kit,VEGFR3/FLT4
A11753	MK-2461			***	c-Met (M1250T),c-Met (Y1235D),c-Met (Y1230H)
A14156	AZD2932			****	Flt3,VEGFR-2,c-Kit
A15062	DCC-2618		***	***	c-Kit

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Pazopanib (GW-786034)

Catalog No. A11518
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VEGFR 抑制剂

Pazopanib (GW-786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

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- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Masitinib mesylate

Catalog No. A15152
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KIT/PDGFR 抑制剂

Masitinib mesylate是Kit和PDGFRα/β的新型抑制剂，IC50为200 nM和540 nM/800 nM，对ABL和c-Fms的抑制作用较弱。了解更多

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- Julia M Harrison, .et al. Muscle fiber-type specific terminal Schwann cell pathology leads to sprouting deficits following partial denervation in SOD1 G93A mice, Neurobiol Dis, 2020, Aug 20;145:105052 PMID: 32827689
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AC710 Mesylate

Catalog No. A16246
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710 Mesylate是一种有效的选择性PDGFR家族激酶抑制剂，对于FLT3/KIT/PDGFRα/PDGFRβ的Kd值分别为0.6 nM/1.0 nM/1.3 nM/1.0 nM。了解更多

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Crenolanib (CP-868596)

Catalog No. A11052
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PDGFR/FLT3 抑制剂

Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。了解更多

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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。了解更多

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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CP-673451

Catalog No. A11350
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PDGFRα/β 抑制剂

CP 673451是一种有效的PDGFR-β抑制剂，IC50为1 nM。了解更多

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- Kaori Aoto, .et al. Complex formation between platelet-derived growth factor receptor β and transforming growth factor β receptor regulates the differentiation of mesenchymal stem cells into cancer-associated fibroblasts, Oncotarget, 2018, Sep 25; 9(75): 34090-34102 PMID: 30344924
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Nintedanib esylate

Catalog No. A16197
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RTK 抑制剂

Nintedanib esylate是多种受体酪氨酸激酶（RTK）和非受体酪氨酸激酶（nRTK）的有效抑制剂。了解更多

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- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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TSU-68 (Orantinib, SU6668)

Catalog No. A10953
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PDFGRβ 抑制剂

TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2；不抑制EGFR。了解更多

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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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JI-101

Catalog No. A13545
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VEGFR2/PDGFRβ/EphB4 抑制剂

JI-101是一种具有血管内皮生长因子受体2（VEGFR2），血小板源性生长因子受体β（PDGFRβ）和ephrin B4受体B4（EphB4）的口服活性抑制剂，具有潜在的抗血管生成和抗肿瘤活性。了解更多

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AC710

Catalog No. A15933
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710是一种有效的，具有活性的，选择性血小板衍生的生长因子受体家族激酶抑制剂，具有潜在的抗癌活性。了解更多

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N-Desethyl Sunitinib

Catalog No. A15182
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VEGFR/PDGFRβ/KIT 抑制剂

N-Desethyl Sunitinib是舒尼替尼的主要药理活性代谢产物，是有效的，ATP竞争性VEGFR，PDGFRβ和KIT抑制剂（VEGFR -1，-2，-3的Ki值为2、9、17、8和4 nM。分别为PDGFRβ和KIT）。了解更多

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Dovitinib Dilactic acid (TKI258 Dilactic acid)

Catalog No. A10198
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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TAK-593

Catalog No. A13555
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VEGFR/PDGFR 抑制剂

TAK-5933是一种口服制剂，其中含有血管内皮生长因子受体（VEGFR）和血小板衍生生长因子受体（PDGFR）的小分子受体酪氨酸激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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R1530

Catalog No. A13111
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Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂

R1530是吡唑并苯并二氮杂小分子，具有潜在的抗血管生成和抗肿瘤活性。R1530也是一种有丝分裂-血管生成抑制剂(MAI),可抑制多种参与血管生成的受体酪氨酸激酶，如血管内皮生长因子受体(VEGFR)-1，-2，-3，血小板衍生生长因子受体(PDGFR)βFMS样酪氨酸激酶(Flt)-3和成纤维细胞生长因子受体(FGFR) -1，-2。了解更多

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Regorafenib monohydrate

Catalog No. A15218
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Tyrosine kinase 抑制剂

Regorafenib monohydrate是VEGFR1/VEGFR2/VEGFR3/PDGFRβ/Kit/RET和Raf-1的多靶点抑制剂，IC50分别为13 nM/4.2 nM/46 nM/22 nM/7 nM/1.5 nM和2.5 nM。了解更多

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