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Apatinib (YN968D1)

Apatinib (YN968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.

Catalog No.S2221

: Tel: +1-832-582-8158[email protected]

Apatinib (YN968D1) Chemical Structure
Molecular Weight: 493.58

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Apatinib (YN968D1) is available in the following compound libraries:

Chemical Library (96-well) FDA Approved Drug Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well)

Product Information

Compare VEGFR Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1040	Sorafenib (Nexavar)	<1 mg/mL	127 mg/mL	<1 mg/mL
S1042	Sunitinib Malate (Sutent)	<1 mg/mL	15 mg/mL	<1 mg/mL
S1490	Ponatinib (AP24534)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1178	Regorafenib (BAY 73-4506)	<1 mg/mL	97 mg/mL	<1 mg/mL
S1119	XL-184 free base (Cabozantinib)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1010	BIBF1120 (Vargatef)	<1 mg/mL	6 mg/mL	3 mg/mL
S1046	Vandetanib (Zactima)	<1 mg/mL	4 mg/mL	<1 mg/mL
S1035	Pazopanib HCl	<1 mg/mL	17 mg/mL	<1 mg/mL
S1005	Axitinib	<1 mg/mL	1 mg/mL	<1 mg/mL
S1264	PD173074	<1 mg/mL	105 mg/mL	105 mg/mL
S1111	Foretinib (GSK1363089, XL880)	<1 mg/mL	127 mg/mL	<1 mg/mL
S1018	Dovitinib (TKI-258)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1017	Cediranib (AZD2171)	<1 mg/mL	90 mg/mL	<1 mg/mL
S2161	RAF265 (CHIR-265)	<1 mg/mL	104 mg/mL	33 mg/mL
S1207	Tivozanib (AV-951)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1470	TSU-68 (SU6668)	<1 mg/mL	62 mg/mL	<1 mg/mL
S1084	Brivanib (BMS-540215)	<1 mg/mL	74 mg/mL	3 mg/mL
S1164	E7080 (Lenvatinib)	<1 mg/mL	40 mg/mL	<1 mg/mL
S1003	Linifanib (ABT-869)	<1 mg/mL	75 mg/mL	<1 mg/mL
S1101	Vatalanib 2HCl (PTK787)	10 mg/mL	85 mg/mL	6 mg/mL
S1361	MGCD-265	<1 mg/mL	104 mg/mL	<1 mg/mL
S2842	SAR131675	<1 mg/mL	30 mg/mL	<1 mg/mL
S1032	Motesanib Diphosphate (AMG-706)	114 mg/mL	114 mg/mL	<1 mg/mL
S2202	NVP-BHG712	<1 mg/mL	101 mg/mL	3 mg/mL
S2769	Dovitinib Dilactic acid (TKI258 Dilactic acid)	70 mg/mL	90 mg/mL	<1 mg/mL
S1181	ENMD-2076	1 mg/mL	105 mg/mL	<1 mg/mL
S2859	Golvatinib (E7050)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1171	CYC116	<1 mg/mL	24 mg/mL	<1 mg/mL
S1220	OSI-930	<1 mg/mL	89 mg/mL	3 mg/mL
S1363	Ki8751	<1 mg/mL	47 mg/mL	<1 mg/mL
S2231	Telatinib (BAY 57-9352)	<1 mg/mL	82 mg/mL	1 mg/mL
S1138	Brivanib alaninate (BMS-582664)	<1 mg/mL	88 mg/mL	88 mg/mL
S1486	AEE788 (NVP-AEE788)	<1 mg/mL	88 mg/mL	<1 mg/mL
S1557	KRN 633	<1 mg/mL	9 mg/mL	<1 mg/mL
S2221	Apatinib (YN968D1)	<1 mg/mL	22 mg/mL	<1 mg/mL
S2896	ZM 323881 HCl	<1 mg/mL	10 mg/mL	<1 mg/mL
S2201	BMS 794833	<1 mg/mL	94 mg/mL	<1 mg/mL
S2200	Raf265 derivative	<1 mg/mL	101 mg/mL	101 mg/mL
S2845	Semaxanib (SU5416)	<1 mg/mL	22 mg/mL	2 mg/mL
S2897	ZM 306416	<1 mg/mL	67 mg/mL	<1 mg/mL
S4001	Cabozantinib malate	<1 mg/mL	127 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	Apatinib (YN968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.
Targets	VEGFR2
IC50	1 nM ^[1]
In vitro	Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGF2. Apatinib can also potently suppress the activities of Ret, c-kit and c-src with IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). Apatinib effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. ^[1] Apatinib reverses ABCB1- and ABCG2-mediated MDR by inhibiting their transport function, but not by blocking the AKT or ERK1/2 pathway or downregulating ABCB1 or ABCG2 expression. Apatinib significantly potentiates the cytotoxicity of established ABCB1 and ABCG2 substrates and increased the accumulation of DOX and Rho 123 in ABCB1- or ABCG2-overexpressing cells. Furthermore, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [¹²⁵I]iodoarylazidoprazosin in a concentration-dependent manner. ^[2]
In vivo	Apatinib inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner. ^[1] Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model. ^[2] Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts. ^[3]
Clinical Trials	Apatinib is in phase III clinical development.
Features	Apatinib (YN968D1) shows good anti-cancer effects for gastric and colorectal cancer compared with sorafenib and sunitinib.

Protocol(Only for Reference)

Kinase Assay: ^[1]

Enzyme-linked immunosorbent assay	A poly(glu, ala, tyr) 6:3:1 random copolymer is used as a tyrosine containing substrate solution. The substrate is stored as a 1 mg/mL stock in PBS at −20 °C and diluted 1 in 500 with PBS in order to coat 96 well plates (100 μL/well). Plates are coated on the day prior to assay, sealed with adhesive seals, and stored overnight at 4 °C. On the day of the assay, the substrate solution is discarded and the assay plate wells are washed once with PBST (PBS containing 0.05% v/v Tween 20) and once with Hepes buffer (50 mM, pH 7.4). Test compounds are diluted with 10% dimethylsulfoxide (DMSO) de-ionized water and 25 μL volumes transferred to wells in the washed assay plates. Manganese chloride solution (40 mM) containing 8 μM ATP is then added (25 μL) to all test wells. Control and blank wells, containing compound diluent and manganese chloride solution with and without ATP, respectively, are also included to determine the dynamic range of the assay. Freshly diluted enzyme (50 μL) is added to each well, and the plates incubated at room temperature for 20 min. The liquid is then discarded and the wells are washed twice with PBST. Mouse IgG anti-phosphotyrosine antibody diluted 1:6000 with PBST containing 0.5% (w/v) bovine serum albumin (BSA) is added (100 μL/well), and the plates incubated for 1h at room temperature before discarding the liquid and washing the wells twice with PBST. Horseradish peroxidase (HRP)-linked sheep anti-mouse Ig antibody diluted 1:500 with PBST containing 0.5% (w/v) BSA, is then added (100 μL/well) and the plates incubated for a further 1 h at room temperature before discarding the liquid and washing the wells twice with PBST. A 1 mg/mL solution of 2,2‘-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid is freshly prepared in 50 mM phosphate-citrate buffer (pH5.0) containing 0.03% (w/v) sodium perborate, and 100 μL added to each well. Plates are then incubated for 20−60 min at room temperature until the optical density value of control wells measured at 405 nm is approximately 1.0. IC50 values for compound enzyme inhibition are interpolated using Microcal Origin following subtraction of blank values.

Enzyme-linked immunosorbent assay

A poly(glu, ala, tyr) 6:3:1 random copolymer is used as a tyrosine containing substrate solution. The substrate is stored as a 1 mg/mL stock in PBS at −20 °C and diluted 1 in 500 with PBS in order to coat 96 well plates (100 μL/well). Plates are coated on the day prior to assay, sealed with adhesive seals, and stored overnight at 4 °C. On the day of the assay, the substrate solution is discarded and the assay plate wells are washed once with PBST (PBS containing 0.05% v/v Tween 20) and once with Hepes buffer (50 mM, pH 7.4). Test compounds are diluted with 10% dimethylsulfoxide (DMSO) de-ionized water and 25 μL volumes transferred to wells in the washed assay plates. Manganese chloride solution (40 mM) containing 8 μM ATP is then added (25 μL) to all test wells. Control and blank wells, containing compound diluent and manganese chloride solution with and without ATP, respectively, are also included to determine the dynamic range of the assay. Freshly diluted enzyme (50 μL) is added to each well, and the plates incubated at room temperature for 20 min. The liquid is then discarded and the wells are washed twice with PBST. Mouse IgG anti-phosphotyrosine antibody diluted 1:6000 with PBST containing 0.5% (w/v) bovine serum albumin (BSA) is added (100 μL/well), and the plates incubated for 1h at room temperature before discarding the liquid and washing the wells twice with PBST. Horseradish peroxidase (HRP)-linked sheep anti-mouse Ig antibody diluted 1:500 with PBST containing 0.5% (w/v) BSA, is then added (100 μL/well) and the plates incubated for a further 1 h at room temperature before discarding the liquid and washing the wells twice with PBST. A 1 mg/mL solution of 2,2‘-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid is freshly prepared in 50 mM phosphate-citrate buffer (pH5.0) containing 0.03% (w/v) sodium perborate, and 100 μL added to each well. Plates are then incubated for 20−60 min at room temperature until the optical density value of control wells measured at 405 nm is approximately 1.0. IC50 values for compound enzyme inhibition are interpolated using Microcal Origin following subtraction of blank values.

Animal Study: ^[1]

Animal Models	Ls174t, HCT 116, SGC-7901, HT-29, A549, NCI-H460 xenografted BALB/cA nude mice
Formulation	0.5% (w/v) carboxymethyl cellulose
Dosages	50, 100, 200 mg/kg
Administration	p.o.

References

Chemical Information

Download Apatinib (YN968D1) SDF

Molecular Weight (MW)	493.58
Formula	C₂₅H₂₇N₅O₄S
CAS No.	811803-05-1
Synonyms	N/A

Solubility (25°C) DMSO 22 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Related VEGFR Inhibitors

Linifanib (ABT-869)

Linifanib (ABT-869) is a novel, potent ATP-competitive RTK inhibitor for KDR, CSF-1R, Flt-1, Flt-3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM, 3 nM, and 66 nM respectively.
BIBF1120 (Vargatef)

BIBF1120 (Vargatef) is a potent inhibitor of VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Cediranib (AZD2171)

Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor with IC50 of 0.5 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.
Dovitinib (TKI-258)

Dovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively.
Motesanib Diphosphate (AMG-706)
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3, PDGFR, c-Kit and Ret with IC50 of 2 nM/3 nM/6 nM, 84 nM, 8 nM and 59 nM, respectively.
Brivanib (BMS-540215)

Brivanib is an ATP-competitive inhibitor against human VEGFR2 and FGFR with IC50 of 25 nM and 148 nM, respectively.
Vatalanib 2HCl (PTK787)

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR, Flt-1 and c-Kit with IC50 of 37 nM, 77 nM and 730 nM, respectively.
Foretinib (GSK1363089, XL880)

XL880 (GSK1363089, EXEL-2880) is an ATP-competitive inhibitor of MET and KDR with IC50 of 0.4 nM and 0.9 nM, respectively.
Brivanib alaninate (BMS-582664)

BMS-582664 is an oral VEGFR/FGFR inhibitor for VEGFR2, Flk1, VEGFR1 and FGFR1 with IC50 of 25 nM, 89 nM, 380 nM and 148 nM, respectively.
E7080 (Lenvatinib)
E7080 (Lenvatinib) is a multi-target inhibitor of VEGFR2 and VEGFR3 with IC50 of 4 nM and 5.2 nM, respectively.

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Apatinib (YN968D1)