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Chemical Structure| 1313725-88-0 Chemical Structure| 1313725-88-0

Structure of Savolitinib
CAS No.: 1313725-88-0

Chemical Structure| 1313725-88-0

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Savolitinib is an orally bioavailable inhibitor of the c-Met receptor tyrosine kinase (IC50= 5 nM) with potential antineoplastic activity.

Synonyms: Volitinib; HMPL-504; HMPL0-504

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Product Details of Savolitinib

CAS No. :1313725-88-0
Formula : C17H15N9
M.W : 345.36
SMILES Code : CN1N=CC(C2=CN=C3C(N([C@H](C4=CN5C(C=C4)=NC=C5)C)N=N3)=N2)=C1
Synonyms :
Volitinib; HMPL-504; HMPL0-504
MDL No. :MFCD28359096
InChI Key :XYDNMOZJKOGZLS-NSHDSACASA-N
Pubchem ID :68289010

Safety of Savolitinib

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

Related Pathways of Savolitinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
OE33 1, 10, 100 nM 24 hours To evaluate the inhibitory effects of Savolitinib on MET and downstream signaling molecules PMC11173193
MKN-45 1, 10, 100 nM 24 hours To evaluate the inhibitory effects of Savolitinib on MET and downstream signaling molecules PMC11173193
PC9 cells 1 μM 72 hours To evaluate the sensitivity of TPR-METWT and TPR-METD1228V to Gefitinib in combination with Savolitinib or Cabozantinib PMC5140694

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice EGFR mutation-positive, MET-amplified NSCLC PDX model Oral 0.3-15 mg/kg Once daily for 20 days To evaluate the antitumor activity of Savolitinib in combination with Osimertinib. Results showed that Savolitinib monotherapy at 15 mg/kg demonstrated significant antitumor activity (84% TGI), while combination therapy showed dose-dependent antitumor activity ranging from 81% TGI (0.3 mg/kg) to 84% tumor regression (15 mg/kg). PMC10157363
Mice Lung cancer model with EGFR mutation and MET gene amplification Oral 15 mg/kg Once daily for 28 days To evaluate the antitumor activity of savolitinib in combination with osimertinib, showing a tumor inhibition rate of 84% PMC11225044
Mice Patient-derived xenograft (PDX) model of NSCLC brain metastases Oral gavage 2.5 mg/kg Twice daily for 2 weeks To evaluate the therapeutic effect of Savolitinib on MET exon 14 mutated NSCLC PDX model, results showed that Savolitinib significantly inhibited tumor growth and enhanced radiation response when combined with radiotherapy. PMC7843608

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02897479 Lung Sarcomatoid Carcinoma PHASE2 UNKNOWN 2021-12-30 Beijing Cancer Hopspital, Beij... More >>ing, Beijing, China|Shanghai Chest Hospital, Shanghai, Shanghai, 210000, China Less <<
NCT03592641 Colorectal Carcinoma|Metastati... More >>c Colon Adenocarcinoma|Metastatic Rectal Adenocarcinoma|Stage III Colon Cancer AJCC v8|Stage III Rectal Cancer AJCC v8|Stage IIIA Colon Cancer AJCC v8|Stage IIIA Rectal Cancer AJCC v8|Stage IIIB Colon Cancer AJCC v8|Stage IIIB Rectal Cancer AJCC v8|Stage IIIC Colon Cancer AJCC v8|Stage IIIC Rectal Cancer AJCC v8|Stage IV Colon Cancer AJCC v8|Stage IV Rectal Cancer AJCC v8|Stage IVA Colon Cancer AJCC v8|Stage IVA Rectal Cancer AJCC v8|Stage IVB Colon Cancer AJCC v8|Stage IVB Rectal Cancer AJCC v8|Stage IVC Colon Cancer AJCC v8|Stage IVC Rectal Cancer AJCC v8|Unresectable Colon Adenocarcinoma|Unresectable Rectal Adenocarcinoma Less << PHASE2 TERMINATED 2021-12-30 Los Angeles County-USC Medical... More >> Center, Los Angeles, California, 90033, United States|USC / Norris Comprehensive Cancer Center, Los Angeles, California, 90033, United States|University of California Davis Comprehensive Cancer Center, Sacramento, California, 95817, United States|Smilow Cancer Hospital-Derby Care Center, Derby, Connecticut, 06418, United States|Smilow Cancer Hospital Care Center-Fairfield, Fairfield, Connecticut, 06824, United States|Smilow Cancer Hospital Care Center - Guilford, Guilford, Connecticut, 06437, United States|Smilow Cancer Hospital Care Center at Saint Francis, Hartford, Connecticut, 06105, United States|Smilow Cancer Center/Yale-New Haven Hospital, New Haven, Connecticut, 06510, United States|Yale University, New Haven, Connecticut, 06520, United States|Yale-New Haven Hospital North Haven Medical Center, North Haven, Connecticut, 06473, United States|Smilow Cancer Hospital-Orange Care Center, Orange, Connecticut, 06477, United States|Smilow Cancer Hospital-Torrington Care Center, Torrington, Connecticut, 06790, United States|Smilow Cancer Hospital Care Center-Trumbull, Trumbull, Connecticut, 06611, United States|Smilow Cancer Hospital-Waterbury Care Center, Waterbury, Connecticut, 06708, United States|Smilow Cancer Hospital Care Center - Waterford, Waterford, Connecticut, 06385, United States|University of Florida Health Science Center - Gainesville, Gainesville, Florida, 32610, United States|Northwestern University, Chicago, Illinois, 60611, United States|University of Chicago Comprehensive Cancer Center, Chicago, Illinois, 60637, United States|University of Kansas Clinical Research Center, Fairway, Kansas, 66205, United States|University of Kansas Cancer Center, Kansas City, Kansas, 66160, United States|University of Kansas Hospital-Westwood Cancer Center, Westwood, Kansas, 66205, United States|University of Kentucky/Markey Cancer Center, Lexington, Kentucky, 40536, United States|Siteman Cancer Center at West County Hospital, Creve Coeur, Missouri, 63141, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|Siteman Cancer Center-South County, Saint Louis, Missouri, 63129, United States|Siteman Cancer Center at Christian Hospital, Saint Louis, Missouri, 63136, United States|Siteman Cancer Center at Saint Peters Hospital, Saint Peters, Missouri, 63376, United States|NYU Winthrop Hospital, Mineola, New York, 11501, United States|Bellevue Hospital Center, New York, New York, 10016, United States|Laura and Isaac Perlmutter Cancer Center at NYU Langone, New York, New York, 10016, United States|Duke University Medical Center, Durham, North Carolina, 27710, United States|Parkland Memorial Hospital, Dallas, Texas, 75235, United States|UT Southwestern/Simmons Cancer Center-Dallas, Dallas, Texas, 75390, United States Less <<
NCT04923945 Non-small Cell Lung Cancer Met... More >>astatic Less << PHASE3 UNKNOWN 2025-12-24 Shanghai Chest Hospital, Shang... More >>hai, Shanghai, 210000, China Less <<
NCT04923932 Gastric Cancer|Esophagogastric... More >> Junction Disorder Less << PHASE2 RECRUITING 2025-10-25 Beijing Cancer Hopspital, Beij... More >>ing, Beijing, China Less <<
NCT02017236 Food Effect|Health Subjects PHASE1 COMPLETED 2025-06-14 Shanghai Xuhui Central Hospita... More >>l, Shanghai, Shanghai, 200031, China Less <<
NCT02449551 Advanced Gastric Adenocarcinom... More >>a Less << PHASE2 COMPLETED 2021-08-27 Samsung Medical center, Seoul,... More >> 135-710, Korea, Republic of Less <<
NCT01773018 Tumor PHASE1 COMPLETED 2025-05-16 Sir Charles Gairdner Hospital,... More >> Nedlands, Western Australia, 6009, Australia|Southern Health and Monash Institute of Medical Research, Clayton, 3168, Australia|Austin Health, Melbourne, 3084, Australia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.48mL

2.90mL

1.45mL

28.96mL

5.79mL

2.90mL

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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