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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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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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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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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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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AP24534 (Ponatinib)

Catalog No. A10080
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BCR-ABL 抑制剂

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。了解更多

Product Citations (6)

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- 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
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- 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
- 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