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Fruquintinib (HMPL-013) VEGFR inhibitor

Name: Fruquintinib (HMPL-013)
Brand: Selleck Chemicals
SKU: S5667
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S5667

Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.

Chemical Structure

Molecular Weight: 393.39

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	EGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2 Bcr-Abl
Other VEGFR Inhibitors	SAR131675 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Linifanib (ABT-869) Anlotinib (AL3818) Dihydrochloride Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl Semaxanib (SU5416)

Solubility

In vitro
Batch:

DMSO : 6 mg/mL (15.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

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.
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.	0.650mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 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.	0.650mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 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.

Chemical Information, Storage & Stability

Molecular Weight	393.39	Formula	C₂₁H₁₉N₃O₅	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1194506-26-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	HMPL-013			Smiles	CC1=C(C2=C(O1)C=C(C=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC)C(=O)NC

Mechanism of Action

Targets/IC₅₀/Ki	VEGFR3 (Cell-free assay) 0.5 nM VEGFR1 (Cell-free assay) 33 nM VEGFR2 (Cell-free assay) 35 nM
In vitro	In in vitro enzymatic and cellular assays, Fruquintinib inhibits VEGFR family kinases and suppressed VEGF/VEGFR cell signaling in human umbilical vein endothelial cell (HUVEC) and human lymphatic endothial cell (HLEC) with IC50 at low nanomolar level. Few kinases are inhibited other than VEGFRs in a panel of 253 kinases test. This compound is a highly potent inhibitor of VEGF-induced angiogenesis.
In vivo	Fruquintinib demonstrates favorable pharmacokinetic profile in multiple animal species, oral administration of this compound strongly suppressed VEGF-induced VEGFR2 phosphorylation in the lung tissue in mice. The extent and duration of the inhibition of VEGFR2 phosphorylation correlated well with drug exposures. The strong anti-angiogenic effect resulted in robust anti-tumor efficacy in a number of human tumor xenograft models with good dose response.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25482937/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04577963	Active not recruiting	Triple Negative Breast Cancer\|Endometrial Cancer\|Solid Tumor Unspecified Adult\|Colorectal Cancer	Hutchison Medipharma Limited\|BeiGene\|Hutchmed	August 9 2021	Phase 1\|Phase 2
NCT04716634	Completed	Advanced Solid Tumors	BeiGene\|Hutchison Medipharma Limited	April 19 2021	Phase 2
NCT04557397	Completed	Drug Drug Interaction	Hutchison Medipharma Limited\|Covance\|Hutchmed	September 2 2020	Phase 1
NCT04322539	Active not recruiting	Metastatic Colorectal Cancer\|Metastatic Colon Cancer	Hutchison Medipharma Limited\|Hutchmed	August 12 2020	Phase 3

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