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Chemical Structure| 1703793-34-3 Chemical Structure| 1703793-34-3

Structure of Avapritinib
CAS No.: 1703793-34-3

Chemical Structure| 1703793-34-3

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BLU-285 is a potent KIT receptor and PDGFRα dual inhibitor with IC50 of 0.27 and 0.24 nM for KIT (D816V) and PDGFRα (D842V) respectively, developed as a highly targeted therapy for SM.

Synonyms: BLU-285

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Product Details of Avapritinib

CAS No. :1703793-34-3
Formula : C26H27FN10
M.W : 498.56
SMILES Code : N[C@@](C)(C1=CC=C(F)C=C1)C2=CN=C(N3CCN(C4=NC=NN5C4=CC(C6=CN(C)N=C6)=C5)CC3)N=C2
Synonyms :
BLU-285
MDL No. :MFCD31544325
InChI Key :DWYRIWUZIJHQKQ-SANMLTNESA-N
Pubchem ID :118023034

Safety of Avapritinib

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

Related Pathways of Avapritinib

RTK

Isoform Comparison

Biological Activity

Target
  • PDGFRα

    PDGFRα (D842V), IC50:0.5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
PDGFRA D842V PDX cells 100 nM 24 h Evaluate the effect of ML-7 and Avapritinib on the cytoskeleton PMC10239357
GIST882 120 nM 120 h Evaluate the effects of MK-1775 and avapritinib on three-dimensional spheroid growth. Results showed that combination treatment significantly reduced spheroid viability and volume. PMC7934848
GIST-T1+D842V KITKO 103.8 nM 72 h Evaluate the effects of MK-1775 and avapritinib on cell cycle and apoptosis. Results showed that MK-1775 induced G0/G1-phase arrest, while avapritinib induced G2 arrest. Combination treatment significantly increased the subG1 population, indicating increased apoptosis. PMC7934848
GIST-T1+Cas9 19.6 Nm 72 h Evaluate the effects of MK-1775 and avapritinib on cell cycle and apoptosis. Results showed that MK-1775 induced G2 phase cell cycle arrest, while avapritinib induced G0/G1-phase arrest. Combination treatment significantly increased the subG1 population, indicating increased apoptosis. PMC7934848
GIST T1 cells 100 nM 24 or 48 h Evaluate the effect of Avapritinib on GIST T1 cell viability and MYLK upregulation PMC10239357
S1-M1-80 0.1 – 1.0 μM 72 h avapritinib reversed ABCG2-mediated mitoxantrone resistance PMC6620786
KB-3-1 0.1 – 1.0 μM 72 h avapritinib resensitized ABCB1-overexpressing KB-V1 cancer cells to paclitaxel at non-toxic concentrations PMC6620786
HEK293 20 μM To evaluate the effect of avapritinib on the drug transport function of ABCB1 and ABCG2 PMC6620786

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C.B17 SCID mice GIST-T1+Cas9 and GIST-T1+D842V KITKO xenograft models Oral 10 mg/kg Daily administration until tumor volume exceeded 10% of body weight or animals demonstrated distress or weight loss greater than 10%. Evaluate the effects of MK-1775 and avapritinib combination therapy on tumor growth and survival. Results showed that combination treatment significantly inhibited tumor growth and induced tumor regression in the GIST-T1+D842V KITKO model. Combination treatment significantly prolonged survival. PMC7934848
NSG mice PDGFRA D842V-mutant GIST xenograft model Oral gavage 3, 10 or 30 mg/kg Once daily for 2 weeks Evaluate the effect of Avapritinib alone or in combination with ML-7 on tumor volume and signaling pathways PMC10239357
Mice H3.3K27M/p53LOF/PDGFRAWT (KPP) model Oral administration 30 mg/kg 15 consecutive days Evaluation of the therapeutic effect of avapritinib on the KPP model showed that avapritinib significantly extended survival (median survival 18 days vs. 26 days, P=0.0023). PMC10326601

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03465722 GIST Phase 3 Recruiting April 2023 -
NCT03731260 Indolent Systemic Mastocytosis... More >> Smoldering Systemic Mastocytosis Less << Phase 2 Not yet recruiting November 2023 -
NCT02508532 Gastrointestinal Stromal Tumor... More >>s (GIST)|Other Relapsed or Refractory Solid Tumors Less << PHASE1 COMPLETED 2021-06-03 Scottsdale Healthcare Hospital... More >>s DBA HonorHealth, Scottsdale, Arizona, 85258, United States|Sarcoma Oncology Center, Santa Monica, California, 90403, United States|Sylvester Comprehensive Cancer Center, Miami, Florida, 33136, United States|Cancer Treatment Centers of America, Atlanta, Georgia, 30256, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Oregon Health and Science University, Portland, Oregon, 97239, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, 19111, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|Leuven Cancer Institute University Hospitals Leuven, Leuven, 3000, Belgium|Centre Leon Berard, Lyon, 69008, France|Institut Gustave Roussy, Paris, 94805, France|University of Duisburg-Essen, Essen, 45122, Germany|Fondazione IRCCS - Istituto Nazinale dei Tumori, Milan, 20133, Italy|Asan Medical Center, Seoul, 05505, Korea, Republic of|Erasmus MC Cancer Institute, Rotterdam, 3015, Netherlands|Centrum Onkologii-Instytut im. Marii Sk?odowskiej-Curie w Warszawie, Warsaw, 02-781, Poland|Vall d' Hebron Institute of Oncology (VHIO), Barcelona, 08305, Spain|Royal Marsden Hospital, London, SW3 6JJ, United Kingdom Less <<
NCT02561988 Aggressive Systemic Mastocytos... More >>is|Systemic Mastocytosis-associated Hematologic Non-mast Cell Disease|Mast Cell Leukemia|Relapsed or Refractory Myeloid Malignancies Less << PHASE1 COMPLETED 2023-01-19 Stanford Cancer Institute, Sta... More >>nford, California, 94305, United States|University of Colorado Cancer Center, Denver, Colorado, 80045, United States|Emory University, Atlanta, Georgia, 30322, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|University of Michigan Health System, Ann Arbor, Michigan, 48109, United States|Mount Sinai Hospital, New York, New York, 10029, United States|University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|Huntsman Cancer Institute, Salt Lake City, Utah, 84112, United States|Beatson West of Scotland Cancer Centre, Glasgow, G12 0XL, United Kingdom|Guy's Hospital, London, SE1 9RT, United Kingdom Less <<
NCT03580655 Advanced Systemic Mastocytosis... More >>|Aggressive Systemic Mastocytosis|Systemic Mastocytosis With an Associated Hematologic Neoplasm|Mast Cell Leukemia Less << PHASE2 ACTIVE_NOT_RECRUITING 2026-01-31 Stanford Cancer Institute, Sta... More >>nford, California, 94305, United States|Rush University Medical Center, Chicago, Illinois, 60612, United States|The University of Kansas Cancer Center, Westwood, Kansas, 66205, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|University of Michigan, Ann Arbor, Michigan, 48109, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|Roswell Park Comprehensive Cancer Center, Buffalo, New York, 14263, United States|Herbert Irving Comprehensive Cancer Center, New York, New York, 10032, United States|University of Pennsylvania, Abramson Cancer Center, Philadelphia, Pennsylvania, 19104, United States|University of Texas, MD Anderson Cancer Center, Houston, Texas, 77030, United States|Mays Cancer Center, San Antonio, Texas, 78229, United States|Huntsman Cancer Institute, Salt Lake City, Utah, 84112, United States|Medizinische Universit?t Wien, Universit?tsklinik für Innere Medizin I, Klinische Abteilung für H?matologie und H?mostaseologie, Vienna, 1090, Austria|St. Michael's Hospital, Toronto, Ontario, M5B 1W8, Canada|Odense University Hospital, Department of Haematology, Odense, DK-5000, Denmark|H?pital Necker-Enfants Malades, Paris, 75015, France|CHU Toulouse - H?pital Larrey, Toulouse, 31059, France|Uniklinik RWTH Aachen, Klinik für H?matologie, Onkologie, H?mostaseologie und Stammzelltranslplantation, Aachen, 52074, Germany|Universit?tsklinikum Hamburg-Eppendorf, Zentrum für Onkologie, Hamburg, 20246, Germany|Universit?tsklinikum Leipzig, Medizinische Klinik und Poliklinik I - H?matologie und Zelltherapie, lnternistische Onkologie, H?mostaseologie, Leipzig, 04103, Germany|Universit?tsmedizin Mannheim III. Medizinische Klinik, Mannheim, 68167, Germany|Klinik und Poliklinik für Innere Medizin III, Klinikum rechts der Isar der TU München, Munich, 81675, Germany|Azienda Ospedaliero-Universitaria Careggi, CRIMM - Centro di Ricerca ed Innovazione per le Malattie Mieloproliferative, Florence, 50134, Italy|A.O. OO.RR. S.Giovanni di Dio e Ruggi d'Aragona, University of Salerno, Salerno, 84131, Italy|Centro Ricerche Cliniche di Verona - Azienda Ospedaliera Universitaria Integrata di Verona, Verona, 37134, Italy|University Medical Center Groningen (UMCG), Groningen, 9713 GZ, Netherlands|Oslo University Hospital-Rikshospitalet, Hematology, Oslo, 0372, Norway|Uniwersyteckie Centrum Kliniczne, Klinika Hematologii i Transplantologii, Gdańsk, 80-214, Poland|Uniwersytecki Szpital Kliniczny im. Jana Mikulicza-Radeckiego we Wroc?awiu, Klinice Hematologii, Nowotworów Krwi i Transplantacji Szpiku, Wroc?aw, 50-367, Poland|lnstituto de Estudios de Mastocitosis de Castilla la Mancha, Hospital Virgen del Valle - Complejo Hospitalario de Toledo, Toledo, 45071, Spain|Beatson West of Scotland Cancer Centre - NHS Greater Glasgow and Clyde, Glasgow, G12 0YN, United Kingdom|Guy's and St Thomas' NHS Foundation Trust - Guy's Hospital, London, SE1 9RT, United Kingdom Less <<
NCT04771520 Anatomic Stage IV Breast Cance... More >>r AJCC V8|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC V8|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC V8|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC V8|Locally Advanced Malignant Solid Neoplasm|Locally Advanced Melanoma|Locally Advanced Primary Malignant Central Nervous System Neoplasm|Locally Advanced Sarcoma|Metastatic Malignant Solid Neoplasm|Metastatic Melanoma|Metastatic Primary Malignant Central Nervous System Neoplasm|Metastatic Sarcoma|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC V8|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC V8|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC V8|Postneoadjuvant Therapy Stage IV Gastroesophageal Junction Adenocarcinoma AJCC V8|Postneoadjuvant Therapy Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC V8|Postneoadjuvant Therapy Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC V8|Prognostic Stage IIIC Breast Cancer AJCC V8|Prognostic Stage IV Breast Cancer AJCC V8|Stage IIIC Colorectal Cancer AJCC V8|Stage IIIC Lung Cancer AJCC V8|Stage IV Colorectal Cancer AJCC V8|Stage IV Lung Cancer AJCC V8|Stage IVA Colorectal Cancer AJCC V8|Stage IVA Lung Cancer AJCC V8|Stage IVB Colorectal Cancer AJCC V8|Stage IVB Lung Cancer AJCC V8|Stage IVC Colorectal Cancer AJCC V8 Less << PHASE2 RECRUITING 2025-02-03 M D Anderson Cancer Center, Ho... More >>uston, Texas, 77030, United States Less <<
NCT03862885 GIST APPROVED_FOR_MARKETING - -
NCT06765915 AML, Adult PHASE2 NOT_YET_RECRUITING 2028-02-01 Ruijin Hospital of Shanghai Ji... More >>aotong University, Shanghai, Shanghai, China Less <<
NCT04825574 Gastrointestinal Stromal Tumor... More >>s Less << PHASE4 COMPLETED 2023-11-23 Gustave Roussy Cancer Campus G... More >>rand Paris Institut de Cancerologie Gustave-Roussy, Villejuif, Val-de-Marne, 94800, France Less <<
NCT05821738 Core Binding Factor Acute Myel... More >>oid Leukemia|KIT Mutation-Related Tumors Less << PHASE2 RECRUITING 2025-12-31 First Affiliated Hospital of S... More >>oochow University, Suzhou, Jiangsu, 215000, China Less <<
NCT04714086 Solid Tumors NO_LONGER_AVAILABLE - -
NCT06748001 Mastocytosis, Systemic PHASE4 RECRUITING 2027-12-31 Universitair Ziekenhuis Antwer... More >>pen (UZA), Edegem, 2650, Belgium|Erasmus Medisch Centrum, Rotterdam, 3015, Netherlands|Oslo University Hospital, Oslo, 0424, Norway Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.03mL

2.01mL

1.00mL

20.06mL

4.01mL

2.01mL

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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