JYP0322
JYP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC).
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- CAS No.: 2644645-39-4
- Formule: C20H16FN7O3
- Masse moléculaire:421.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
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TrkA |
TrkB |
TrkC |
JYP0322 inhibits wild-type ROS1 and ROS1G2032R with high selectivity, showing 130-fold, 20-fold, and 6-fold selectivity over TRKA, TRKB, and TRKC, respectively[1].
JYP0322 (0-1 μM; 3 days) potently inhibited CD74-ROS1-driven Ba/F3 cells (wild-type and mutants), while showing reduced activity against TRK-driven Ba/F3 LMNA-NTRK1 cells, maintaining ROS1 selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 LMNA-NTRK1; wild-type Ba/F3 cells
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Concentration:0-1 μM
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Incubation Time:3 days
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Result:Showed reduced potency against Ba/F3 LMNA-NTRK1 cells (IC50 = 37 nM) compared to Repotrectinib (HY-103022) (IC50 = 1.1 nM).
Inhibited proliferation of Ba/F3 cells expressing wild-type CD74-ROS1 and clinically relevant ROS1 mutations.
JYP0322 (1, 3, and10 mg/kg; p.o.; twice daily for 5 weeks) induces dose-dependent tumor growth inhibition in mouse LU-01-0414 SDC4-ROS1 PDX xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c Nude mice (6-8 weeks old) subcutaneously injected with CD74-ROS1WT cells[1]
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Dosage:1.5; 5; 15 mg/kg
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Administration:p.o.; BID for 2 weeks
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Result:Achieved tumor growth inhibition (TGI) rates of 83.5%, 101.4%, and 103.4% at doses of 1.5, 5, and 15 mg/kg BID, respectively.
Demonstrated efficacy at 5 mg/kg comparable to Crizotinib (HY-50878).
Caused no significant weight loss or observable adverse effects.
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Animal Model:Female BALB/c Nude mice (6-8 weeks old) subcutaneously implanted with LU-01-0414 SDC4-ROS1 tumor fragments[1]
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Dosage:1; 3; 10 mg/kg
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Administration:p.o.; BID for 5 weeks
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Result:Achieved TGI rates of 87.3% at 3 mg/kg, comparable to Entrectinib (HY-12678).
Achieved TGI rates of 94.2% at 10 mg/kg, comparable to Repotrectinib.
Caused no significant weight loss or observable adverse effects.
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Animal Model:Female NOD SCID mice (6-8 weeks old) subcutaneously injected with Ba/F3 CD74-ROS1G2032R cells[1]
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Dosage:1.5; 5; 15 mg/kg
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Administration:p.o.; BID for 2 weeks
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Result:Induced tumor regression at doses of 5 and 15 mg/kg, achieving TGI rates of 81.7% and 100.3%, respectively.
Demonstrated superior efficacy to Taletrectinib (HY-131003) and Repotrectinib.
Caused no significant weight loss or observable adverse effects.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2644645-39-4
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Masse moléculaire 421.38
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Formule C20H16FN7O3
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SMILES
N#CC1=NN2C=CC3=NC2=C1C(NC4(COC5=NC=C(C=C5[C@H]6CCON36)F)CC4)=O
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Synonyms
ROS1-IN-3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JYP0322 Related Classifications
HY-176942 Related Classifications
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