Apatinib

Catalog No.S2221 Synonyms: YN968D1

Apatinib Chemical Structure

Molecular Weight(MW): 493.58

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

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 320 In stock
USD 970 In stock

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Click to view more

Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Apatinib is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.
Features Good anti-tumor effects for gastric and colorectal cancer compared with sorafenib and sunitinib.
Targets
VEGFR2 [1] RET [1] c-Kit [1] c-Src [1] PDGFRα [1]
1 nM 13 nM 429 nM 530 nM >1 μM
In vitro

Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGFR2. 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]

Protocol

Animal Research
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 22 mg/mL (44.57 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% CMC 6 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 493.58
Formula

C25H27N5O4S

CAS No. 811803-05-1
Storage powder
in solvent
Synonyms YN968D1

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02836171 Recruiting Neoplasms Jiangsu HengRui Medicine Co., Ltd. July 2016 Phase 1
NCT02844881 Not yet recruiting Advanced Solid Tumors|Excluding T Cell Lymphoma The First Peoples Hospital of Lianyungang|HengRui YuanZheng Bio-Technology Co.,Ltd. July 2016 Phase 1|Phase 2
NCT02848794 Not yet recruiting High-grade Glioma The First Peoples Hospital of Lianyungang|Shandong Cancer Hospital and Institute|The Affiliated Hospital of Medical College of Qingdao University|Yankuang Group General Hospital|Lianyungang Hospital Affiliated Bengbu Medical College|Suzhou Kowloon Hospital July 2016 Phase 1|Phase 2
NCT02824458 Recruiting EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors Sun Yat-sen University June 2016 Phase 3
NCT02829385 Recruiting Colorectal Neoplasms Shoucheng Ma|LanZhou University June 2016 Phase 2
NCT02775370 Not yet recruiting Adenoid Cystic Carcinoma Shanghai Ninth Peoples Hospital Affiliated to Shanghai Jiao Tong University June 2016 Phase 2

Tech Support

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

Related VEGFR Products

Tags: buy Apatinib | Apatinib supplier | purchase Apatinib | Apatinib cost | Apatinib manufacturer | order Apatinib | Apatinib distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID