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Chemical Structure| 1874276-76-2 Chemical Structure| 1874276-76-2

Structure of Darovasertib
CAS No.: 1874276-76-2

Chemical Structure| 1874276-76-2

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LXS196 is a potent and orally active protein kinase C (PKC) inhibitor used for the treatment of uveal melanoma.

Synonyms: Lxs196; IDE196

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Product Details of Darovasertib

CAS No. :1874276-76-2
Formula : C22H23F3N8O
M.W : 472.47
SMILES Code : O=C(C1=NC(C2=NC=CC=C2C(F)(F)F)=CN=C1N)NC3=NC=CC=C3N4CCC(C)(N)CC4
Synonyms :
Lxs196; IDE196
MDL No. :MFCD31544328

Safety of Darovasertib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Darovasertib

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293 cells 40 nM 30 minutes Inhibition of PKC-mediated LRRK1 activation, blocking Rab7A phosphorylation PMC9555798
OMM1.3 UM cells 1 μM 24 hours Evaluate the effect of Darovasertib on YAP subcellular localization, showing that Darovasertib partially reduced nuclear localization of YAP. PMC10694608
92.1 UM cells 1 μM 2 hours Evaluate the effect of Darovasertib on phosphorylated FAK and ERK, showing that Darovasertib partially reduced pFAK levels. PMC10694608

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID/NOD mice UM 92.1 xenograft model Oral 50 mg/kg Twice daily for 25 days Evaluate the effect of Darovasertib on tumor growth, showing that Darovasertib partially controlled tumor growth. PMC10694608

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05907954 Uveal Melanoma PHASE2 RECRUITING 2029-01-31 HonorHealth Research Institute... More >>, Scottsdale, Arizona, 85258, United States|Moores Cancer Center, La Jolla, California, 92093, United States|UCLA Medical Center, Los Angeles, California, 90024, United States|Stanford Cancer Institute, Palo Alto, California, 94305, United States|Sarah Cannon Research Institute, Denver, Colorado, 80218, United States|University of Miami, Miami, Florida, 33146, United States|The Cancer and Hematology Centers, Grand Rapids, Michigan, 49546, United States|Mayo Clinic Rochester, Rochester, Minnesota, 55905, United States|Northwell, Manhasset, New York, 11030, United States|Duke University Health System, Durham, North Carolina, 27710, United States|Thomas Jefferson University, Philadelphia, Pennsylvania, 19107, United States|Sarah Cannon Research Institute, Nashville, Tennessee, 37203, United States|University of Texas Southwestern Medical Center, Dallas, Texas, 75390, United States|St. Vincent's Health Sydney, Sydney, New South Wales, 2010, Australia|Alfred Health, Melbourne, Victoria, 3004, Australia|Princess Margaret Cancer Centre, Toronto, Ontario, M5G2M9, Canada|Institute Curie, Paris, 75005, France|Charité - Universit?tsmedizin Berlin, Berlin, 12203, Germany|University Hospital Essen - West German Cancer Center, Essen, 45147, Germany|Fondazione IRCCS Istituto Nazionale Tumori, Milan, 20133, Italy|Instituto Nazionale Tumori IRCCS - Fondazione Pascale, Napoli, 80131, Italy|Fondazione Policlinico Universitario Agostino Gemelli IRCCS, Rome, 00168, Italy|Leiden University Medical Center, Leiden, 2333 ZA, Netherlands|University College London Hospital - NHS Foundation Trust, London, NW1 2PG, United Kingdom|The Clatterbridge Cancer Centre NHS Foundation Trust, Wirral, CH63 4JY, United Kingdom Less <<
NCT05187884 Ocular Melanoma PHASE2 ACTIVE_NOT_RECRUITING 2025-11-01 Kinghorn Cancer Centre, St. Vi... More >>ncent's Hospital, Sydney, New South Wales, 2010, Australia|Alfred Hospital, Melbourne, Victoria, 3004, Australia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.17mL

4.23mL

2.12mL

References

 

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