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Chemical Structure| 1194506-26-7 Chemical Structure| 1194506-26-7

Structure of Fruquintinib
CAS No.: 1194506-26-7

Chemical Structure| 1194506-26-7

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Fruquintinib is an inhibitor of VEGFR family with IC50s of 33 nM, 35 nM and 0.5 nM for VEGFR1, 2, 3 respectively.

Synonyms: HMPL-013

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Product Details of Fruquintinib

CAS No. :1194506-26-7
Formula : C21H19N3O5
M.W : 393.39
SMILES Code : O=C(C1=C(C)OC2=CC(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)=CC=C12)NC
Synonyms :
HMPL-013
MDL No. :MFCD28502149
InChI Key :BALLNEJQLSTPIO-UHFFFAOYSA-N
Pubchem ID :44480399

Safety of Fruquintinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Fruquintinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
COLO 205 cells IC50 >10.0 µM Evaluate the in vitro anticancer activity of Fruquintinib against COLO 205 cells, showing weak activity (IC50 >10.0 µM) PMC9448386
HEK293-KDR cells 0.6 nmol/L Inhibition of VEGF-A dependent KDR phosphorylation PMC4622458
LOVO 0, 50, 100, 150, 200 μM 24, 48, 72 hours Fruquintinib significantly inhibited the proliferation, migration, and invasion of LOVO cells. PMC11932892
HCT-116 0, 50, 100, 150, 200 μM 24, 48, 72 hours Fruquintinib significantly inhibited the proliferation, migration, and invasion of HCT-116 cells. PMC11932892
Macrophages 0.05 μmol/l 24 hours HMPL-013 inhibited VEGF/VEGFR2-induced macrophage M1 polarization. PMC7695853
Human choroidal vascular endothelial cells (HCVECs) 0.05 μmol/l 24 hours HMPL-013 downregulated VEGF/VEGFR2/PI3K/AKT/NF-κB pathway and CCL2 secretion in HCVECs. PMC7695853
HCT-116 cells IC50 >10.0 µM Evaluate the in vitro anticancer activity of Fruquintinib against HCT-116 cells, showing weak activity (IC50 >10.0 µM) PMC9448386
HT-29 cells IC50 >10.0 µM Evaluate the in vitro anticancer activity of Fruquintinib against HT-29 cells, showing weak activity (IC50 >10.0 µM) PMC9448386

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice BGC-823 tumor xenograft model Oral 2.5 mg/kg Single dose Inhibition of VEGF stimulated VEGFR2 phosphorylation PMC4622458
C57BL/6 mice Laser-induced choroidal neovascularization (CNV) model Intravitreal injection 5 μg/μl Single injection, observed for 7 days HMPL-013 alleviated mouse CNV formation without obvious ocular toxicity. PMC7695853
Rat Pharmacokinetic study in rat plasma Oral 1.0 mg/kg Single dose, sampling time points: 0.33, 0.67, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, and 48 hrs To evaluate the pharmacokinetic properties of Fruquintinib in rats. Results showed that Fruquintinib was rapidly absorbed after oral administration, with Cmax reached at 4.25 hrs and t1/2 about 3.34 hrs. PMC6699497

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05025631 Colorectal Cancer PHASE2 COMPLETED 2022-10-30 China West Hospital, Chengdu, ... More >>Sichuan, 610000, China Less <<
NCT05216367 Hepatic Impairment PHASE1 COMPLETED 2022-10-25 Clinical Pharmacology of Miami... More >>, Miami, Florida, 33014-3616, United States|Orlando Clinical Research Center, Orlando, Florida, 32809, United States Less <<
NCT01645215 Tumor PHASE1 COMPLETED 2025-10-12 Fudan University Cancer Center... More >>, Shanghai, Shanghai, 200032, China Less <<
NCT06202599 Bone Sarcoma|Soft Tissue Sarco... More >>ma|Refractory Tumor Less << COMPLETED 2023-11-15 Peking University People's Hos... More >>pital, Beijing, Beijing, 100044, China Less <<
NCT06018714 Colorectal Cancer Metastatic PHASE2 RECRUITING 2026-08-01 Colorectal Department,SunYat-s... More >>en University Cancer Center, Guangzhou, Guangdong, 510062, China Less <<
NCT05257122 Advanced Pancreatic Carcinoma PHASE2 UNKNOWN 2025-02-24 Fudan University Shanghai Canc... More >>er Center, Shanghai, Shanghai, 200032, China Less <<
NCT06202417 Colorectal Cancer|Refractory C... More >>olorectal Cancer|Metastatic Colorectal Cancer Less << COMPLETED 2023-12-25 Zhongshan Hospital, Fudan Univ... More >>ersity, Shanghai, Shanghai, 200032, China Less <<
NCT05142631 Soft Tissue Sarcoma PHASE2 UNKNOWN 2023-08-30 Fudan University Shanghai Canc... More >>er Center, Shanghai, Shanghai, 200032, China Less <<
NCT05447715 Metastatic Colorectal Cancer PHASE2 UNKNOWN 2025-01-31 Fudan University Cancer Hospit... More >>al, ShangHai, Shanghai, 200032, China Less <<
NCT04156958 Biliary Tract Adenocarcinoma PHASE2 UNKNOWN 2025-12-21 Chinese PLA General Hospital 5... More >>th Medical Center, Beijing, Beijing, China|Hebei Tumor Hospital, Shijiazhuang, Hebei, China|Harbin Medical University Cancer Hospital, Harbin, Heilongjiang, China|The Second Xiangya Hospital of Central South University, Changsha, Hunan, China|Jilin Cancer Hospital, Chang chun, Jilin, China|Shanxi Provincial Cancer Hospital, Taiyuan, Shanxi, China|West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China Less <<
NCT06094868 Gastric Cancer PHASE2 NOT_YET_RECRUITING 2025-10-26 -
NCT06562543 Colorectal Cancer PHASE4 RECRUITING 2028-02-18 Central Alabama Research, Birm... More >>ingham, Alabama, 35209, United States|University of Alabama at Birmingham, Birmingham, Alabama, 35249, United States|Ironwood Cancer and Research Centers, Gilbert, Arizona, 85297, United States|University of Arizona, Tucson, Arizona, 85719, United States|University of Southern California, Los Angeles, California, 90033, United States|Christiana Care Health Services, Newark, Delaware, 19713, United States|University of Miami, Miami, Florida, 33146, United States|Baptist Health - Miami Cancer Institute, Miami, Florida, 33176, United States|Emory University, Atlanta, Georgia, 30322, United States|Hope and Healing Cancer Services, Hinsdale, Illinois, 60521, United States|Indiana University, Indianapolis, Indiana, 46202, United States|Our Lady of the Lake Physician Group - LSU Health Baton Rouge Oncology, Baton Rouge, Louisiana, 70805, United States|Willis Knighton Cancer Center, Shreveport, Louisiana, 71103, United States|Mercy Medical Center, Baltimore, Maryland, 21202, United States|Boston Medical Center, Boston, Massachusetts, 02118, United States|Hattiesburg Clinic, Hattiesburg, Mississippi, 39401, United States|Saint Luke's Cancer Institute, Kansas City, Missouri, 64111, United States|Midwest Oncology Associates - Kansas City, Kansas City, Missouri, 64132, United States|SSM Health St. Louis DePaul Hospital, Saint Louis, Missouri, 63044, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|Capital Health Medical Center - Hopewell, Pennington, New Jersey, 08534, United States|Albert Einstein College of Medicine, Bronx, New York, 10461, United States|James J Peters Veterans Administration Medical Center - NAVREF, Bronx, New York, 10468, United States|Hightower Clinical Research, Oklahoma City, Oklahoma, 73102, United States|Jefferson Health, Philadelphia, Pennsylvania, 19107-4247, United States|Fox Chase Cancer Center | Philadelphia, PA, Philadelphia, Pennsylvania, 19111, United States|Medical University of South Carolina, Charleston, South Carolina, 29425, United States|University of Tennessee -- Memphis, Memphis, Tennessee, 38163-2116, United States|Vanderbilt University Medical Center, Nashville, Tennessee, 37212-1610, United States|University of Texas Southwestern Medical Center, Dallas, Texas, 75235-7320, United States|Oncology Consultants - Memorial City Location, Houston, Texas, 77024-2645, United States|Baylor College of Medicine, Houston, Texas, 77030, United States|Renovatio Clinical, Houston, Texas, 77056, United States|Renovatio Clinical, Houston, Texas, 77056, United States|Tranquil Research, Webster, Texas, 77598, United States|UC Irvine Medical Center - Chao Family Comprehensive Cancer, Orange, Virginia, 22960, United States|Virginia Commonwealth University, Richmond, Virginia, 23298-0037, United States|Medstar Speciality Hospital, Northwest, Washington, 20010, United States|Fundacion de Investigacion de Diego (FDI Clinical Research), San Juan, 00927, Puerto Rico Less <<
NCT04296019 Colo-rectal Cancer PHASE2 UNKNOWN 2025-01-01 Zhongshan Hospital Affiliated ... More >>to Fudan University, Shanghai, Shanghai, 200032, China Less <<
NCT06613113 MSS Metastatic Colorectal Canc... More >>er Less << RECRUITING 2027-07-31 Kaitai Liu, Ningbo, Zhejiang, ... More >>315040, China Less <<
NCT06774222 Gastric/Gastroesophageal Junct... More >>ion Adenocarcinoma Less << PHASE2 RECRUITING 2026-12-31 Henan Cancer Hospital, Zhengzh... More >>ou, China Less <<
NCT03684967 Lung Cancer PHASE2 WITHDRAWN 2019-09-06 Guangdong General Hospital, Gu... More >>angzhou, Guangdong, 510060, China Less <<
NCT06446154 Hepatocellular Carcinoma|Immun... More >>e Checkpoint Inhibitors|Anti-angiogenic Therapy|Second-line Treatment Less << PHASE2 RECRUITING 2026-07-01 Sun Yat-sen university cancer ... More >>center, Guangzhou, Guangdong, China Less <<
NCT05216354 Renal Impairment PHASE1 COMPLETED 2023-06-26 Clinical Pharmacology of Miami... More >>, Miami, Florida, 33014-3616, United States|Orlando Clinical Research Center, Orlando, Florida, 32809, United States Less <<
NCT06118762 Metastatic Colorectal Cancer PHASE4 RECRUITING 2026-10-01 The First Affiliated Hospital ... More >>of Nanchang University, Nanchang, Jiangxi, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.71mL

2.54mL

1.27mL

25.42mL

5.08mL

2.54mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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