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Apatinib (YN968D1) VEGFR2 Inhibitor

Cat.No.: S5248

Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signalling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.

Apatinib (YN968D1) VEGFR Inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 397.47

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	EGFR FGFR PDGFR c-Met Src MEK CSF-1R HER2 FLT3 c-Kit
Other VEGFR Inhibitors	SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) mesylate Ki8751 Semaxanib (SU5416) ZM 323881 HCl

Solubility in DMSO or water

In vitro
Batch:

DMSO : 100 mg/mL (251.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 79 mg/mL (198.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 79 mg/mL (198.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : ˂1 mg/mL

The solubility data above are all experimental results (not literature values).

DMSO : 79 mg/mL (198.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 9 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 79 mg/mL (198.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.100mg/ml (10.32mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.300mg/ml (3.27mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.950mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 79 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.450mg/ml (1.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Read more about Apatinib (YN968D1) solubility in DMSO or water

Search by Cell Line | Choose a Research Area to Find Working Concentrations

Read more about Apatinib (YN968D1) working concentrations for cell culture treatment

Apatinib (YN968D1) is a potent inhibitor of VEGFR2 (1 nM), RET (13 nM), VEGFR1 (70 nM), KIT (429 nM), CYP2C9 (440 nM), SRC (530 nM), PDGFRB (537 nM), PDGFRA (>1000 nM), CYP3A4 (1800 nM), EGFR (>10000 nM), HER2 (>10000 nM), FGFR1 (>10000 nM), HLM (480000 nM), RLM (950000 nM). Apatinib (YN968D1) exhibits the greatest inhibitory potency toward VEGFR2 (IC50 = 1 nM).

Selectivity & Specificity Details

Mechanism of Action

Information	Apatinib (YN968D1) is a potent, highly selective, ATP-competitive VEGFR2 inhibitor. It affects VEGF/VEGFR signaling by binding to the intracellular ATP-binding site to prevent receptor phosphorylation, effectively inhibiting tumor angiogenesis and endothelial cell proliferation.
Read more about Apatinib (YN968D1) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about Apatinib (YN968D1) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	397.47	Formula	C₂₄H₂₃N₅O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	811803-05-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Rivoceranib, YN968D1			Smiles	O=C(NC1=CC=C(C=C1)C2(CCCC2)C#N)C3=C(NCC4=CC=NC=C4)N=CC=C3

Read more about storage & stability

Read more comparative analysis about Apatinib (YN968D1)

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 )

*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

Concentration (start):

Dilution-folds:

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):