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Chemical Structure| 1058137-23-7 Chemical Structure| 1058137-23-7

Structure of Lucitanib
CAS No.: 1058137-23-7

Chemical Structure| 1058137-23-7

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E-3810 is a dual inhibitor of the VEGF and FGF receptors, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

Synonyms: E-3810; Lucitanib hydrochloride; AL3810

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Product Details of Lucitanib

CAS No. :1058137-23-7
Formula : C26H25N3O4
M.W : 443.49
SMILES Code : O=C(NC)C1=CC=CC2=C1C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C43)=C2
Synonyms :
E-3810; Lucitanib hydrochloride; AL3810
MDL No. :MFCD20527751
InChI Key :CUDVHEFYRIWYQD-UHFFFAOYSA-N
Pubchem ID :25031915

Safety of Lucitanib

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

Related Pathways of Lucitanib

RTK

Isoform Comparison

Biological Activity

Target
  • FGFR2

    FGFR2, IC50:82.5 nM

  • FGFR1

    FGFR1, IC50:17.5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Baf3-CCDC6-RET cells 1–10 μmol/L AL3810 dose-dependently inhibited the proliferation of Baf3-CCDC6-RET cells with an IC50 value of 2.77 μmol/L. Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542
TPC-1 cells 2–5 μmol/L 72 hours AL3810 dose-dependently inhibited the proliferation of TPC-1 cells with IC50 values ranging from 0.59 to 7.03 μmol/L. Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542
SW579 cells 2–5 μmol/L 72 hours AL3810 dose-dependently inhibited the proliferation of SW579 cells with IC50 values ranging from 0.59 to 7.03 μmol/L. Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542
TT cells 2–5 μmol/L 72 hours AL3810 dose-dependently inhibited the proliferation of TT cells with IC50 values ranging from 0.59 to 7.03 μmol/L. Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542
Small cell lung cancer cell line (DMS114) 1μM 4, 24, 48 and 72 hours To study the effect of Lucitanib on cell cycle in FGFR1 amplified cell lines. Results showed a G1 block in DMS114 cells from 24 to 48 hours, but no apoptosis was detected. Neoplasia. 2017 Jan;19(1):35-42
Non-small cell lung cancer cell lines (H1299, H1975, H2342, H1650, H358, A549, H2228, H23, H1581, H520) 0.01 to 50μM 72 hours To evaluate the growth inhibitory effect of Lucitanib on cell lines with FGFR1/2 amplification or mutation. Results showed that FGFR1/2 amplified or mutated cell lines were more sensitive to Lucitanib (IC50 of 0.045–3.16μM) compared to wild-type cell lines (IC50 of 3–23μM). Neoplasia. 2017 Jan;19(1):35-42
CAMA1 cells 1 μM 6 days Lucitanib combined with fulvestrant/palbociclib significantly inhibited cell growth, inducing cell cycle arrest and senescence Nat Commun. 2019 Mar 26;10(1):1373
T47D cells 1 μM 14 days FGFR1 overexpression confers resistance to fulvestrant ± palbociclib, which was reversed by lucitanib Nat Commun. 2019 Mar 26;10(1):1373
MCF-7 cells 1 μM 14 days FGFR1 overexpression confers resistance to fulvestrant ± palbociclib, which was reversed by lucitanib Nat Commun. 2019 Mar 26;10(1):1373
CAMA1 cells 2 μM 6 hours Inhibited the association of FGFR1 with ERα and reduced ERα-dependent gene transcription Clin Cancer Res. 2017 Oct 15;23(20):6138-6150

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice MCF-7FGFR1 xenograft model Oral 10 mg/kg/day Daily until tumor volume assessment The triple therapy (fulvestrant + palbociclib + lucitanib) significantly inhibited tumor growth in FGFR1-overexpressing tumors, reducing p-RB and p-FGFR1 levels Nat Commun. 2019 Mar 26;10(1):1373
BALB/c nude mice SW579 and TT xenograft models Oral 5–20 mg·kg-1·d-1 Once daily for 21 days AL3810 significantly inhibited tumor growth in SW579 and TT xenograft models and reduced microvessel density in tumor tissues. Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542
Female NCr-nu/nu mice Lung, gastric and endometrial carcinoma xenograft models Oral 2.5, 5, 10 or 20 mg/kg Once daily for 30 days To evaluate the antitumor activity of Lucitanib in FGFR1/2 amplified or mutated tumor models. Results showed dose-dependent tumor growth inhibition in all models, with more significant effects in FGFR1 amplified lung cancer models. Neoplasia. 2017 Jan;19(1):35-42
Female athymic nude mice ER+/HER2-/FGFR1-amplified PDX models Oral 7 mg/kg/day Once daily for 3 weeks Combination of fulvestrant and lucitanib significantly inhibited tumor growth Clin Cancer Res. 2017 Oct 15;23(20):6138-6150

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03117101 Advanced Solid Tumors PHASE1 COMPLETED 2025-09-16 Fudan University Shanghai Canc... More >>er Center, Shanghai, Shanghai, 200000, China Less <<
NCT02747797 Advanced Cancer PHASE2 WITHDRAWN 2025-04-22 UC San Diego Moores Cancer Cen... More >>ter, La Jolla, California, 92093, United States Less <<
NCT02109016 Non-Small Cell Lung Cancer|Squ... More >>amous Non-Small Cell Lung Cancer|NSCLC|Small Cell Lung Cancer|SCLC|Lung Cancer|Advanced Lung Cancer|Metastatic Lung Cancer|Stage IV Lung Cancer Less << PHASE2 TERMINATED 2025-09-16 University of California, Los ... More >>Angeles, Los Angeles, California, 90095, United States|University of Colorado, Aurora, Colorado, 80045, United States|Georgetown University, Washington, District of Columbia, 20007, United States|Emory University, Atlanta, Georgia, 30322, United States|Associates in Oncology and Hematology, Rockville, Maryland, 20850, United States|University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania, 15232, United States|Tennessee Oncology, Nashville, Tennessee, 37203, United States|CHU Caen, H?pital de la C?te de Nacre, Caen, 14033, France|CHRU Lille, H?pital Albert Calmette, Lille, 59037, France|H?pital Nord, Marseille, 13915, France|Institut Gustave-Roussy, Villejuif, 94805, France|Universit?t Duisburg-Essen, Essen, 45147, Germany|Hospital Grosshansdorf, Grosshansdorf, 22927, Germany|Pius Hospital Oldenburg, Oldenburg, 26121, Germany|Ospedale San Raffaele, Milano, 20132, Italy|Fondazione IRCCS Istituto Nazionale Tumori, Milano, 20133, Italy|AOU San Luigi Gonzaga, Orbassano, 10043, Italy|Ospedale S. Maria della Misericordia, Perugia, 06156, Italy|Hospital Universitari Vall d'Hebrón, Barcelona, Catalu?a, 8035, Spain Less <<
NCT02202746 Breast Cancer|Metastatic Breas... More >>t Cancer|MBC|HER2 Positive|HER2|Estrogen Receptor Positive|ER|Triple Negative Less << PHASE2 TERMINATED 2017-01-18 Arizona Oncology Associates, S... More >>edona, Arizona, 86336, United States|Comprehensive Blood and Cancer Center, Bakersfield, California, 93309, United States|Saint Jude Heritage Medical Center, Fullerton, California, 92835, United States|Moores UCSD Cancer Center, La Jolla, California, 92093, United States|University of Southern California, Los Angeles, California, 90033, United States|Cedars-Sinai Medical Center, Los Angeles, California, 90048, United States|University of California, Los Angeles, Los Angeles, California, 90095, United States|Cancer Care Associates Medical Group, Inc., Redondo Beach, California, 90277, United States|University of California San Francisco, San Francisco, California, 94115, United States|Central Coast Medical Oncology Group, Santa Maria, California, 93454, United States|Yale University, New Haven, Connecticut, 06519, United States|University of Miami, Deerfield Beach, Florida, 33442, United States|Memorial West Cancer Center, Hollywood, Florida, 33021, United States|Northwestern University, Robert H. Lurie Comprehensive Cancer Center, Chicago, Illinois, 60611, United States|University of Chicago Medical Center, Chicago, Illinois, 60637, United States|Indiana University Simon Cancer Center, Indianapolis, Indiana, 46202, United States|Horizon Oncology Center, Lafayette, Indiana, 47905, United States|The Sidney Kimmel Comprehensive Cancer Center at John Hopkins, Baltimore, Maryland, 21231, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Comprehensive Cancer Centers of Nevada, Las Vegas, Nevada, 89169, United States|Cooper University Hospital, Voorhees, New Jersey, 08043, United States|Sciode Medical Associates, PLLC, Bronx, New York, 10469, United States|Memorial Sloan-Kettering Cancer Center, New York, New York, 10065, United States|Weill Cornell Breast Center, New York, New York, 10065, United States|University Hospitals Case Medical Center, Cleveland, Ohio, 44106, United States|University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania, 15213, United States|Sarah Cannon Cancer Center, Nashville, Tennessee, 37203, United States|Vanderbilt Ingram Cancer Center, Nashville, Tennessee, 37232, United States|Texas Oncology - Austin Central, Austin, Texas, 78731, United States|Texas Oncology - Baylor Charles A. Sammons Cancer Center, Dallas, Texas, 75246, United States|The Center for Cancer and Blood Disorders, Fort Worth, Texas, 76104, United States|US Oncology, Houston, Texas, 77024, United States|Virginia Oncology Associates, Norfolk, Virginia, 23502, United States Less <<
NCT01283945 Solid Tumors PHASE1|PHASE2 COMPLETED 2017-05-04 Institute Gustave Roussy, Vill... More >>ejuif, Paris, 94805, France|Hopital Louis Pradel, Lyon, 69677, France|European Institute of Oncology, Milano, 20141, Italy|Vall d' Hebron University Hospital, Barcellona, Spain Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.23mL

11.27mL

2.25mL

1.13mL

22.55mL

4.51mL

2.25mL

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

 

Historical Records

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