2. Protein Tyrosine Kinase/RTK Neuronal Signaling
  3. ROS Kinase Trk Receptor
  4. JYP0322

YP0322 (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).

For research use only. We do not sell to patients.

JYP0322

JYP0322 Chemical Structure

CAS No. : 2644645-39-4

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JYP0322 Related Antibodies

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Description

YP0322 (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)[1].

IC50 & Target[1]

TrkA

 

TrkB

 

TrkC

 

In Vitro

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.

JYP0322 Related Antibodies

Cell Viability Assay[1]

Cell Line: Ba/F3 LMNA-NTRK1; wild-type Ba/F3 cells
Concentration: 0-1 μM
Incubation Time: 3 days
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.
In Vivo

JYP0322 (1.5, 5, and 15 mg/kg; p.o.; BID for 2 weeks) inhibits tumor growth in mouse Ba/F3 CD74-ROS1WT and Ba/F3 CD74-ROS1G2032 Rxenografts[1].
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.

Animal Model: Female BALB/c Nude mice (6-8 weeks old) subcutaneously injected with CD74-ROS1WT cells[1]
Dosage: 1.5; 5; 15 mg/kg
Administration: p.o.; BID for 2 weeks
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.
Animal Model: Female BALB/c Nude mice (6-8 weeks old) subcutaneously implanted with LU-01-0414 SDC4-ROS1 tumor fragments[1]
Dosage: 1; 3; 10 mg/kg
Administration: p.o.; BID for 5 weeks
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.
Animal Model: Female NOD SCID mice (6-8 weeks old) subcutaneously injected with Ba/F3 CD74-ROS1G2032R cells[1]
Dosage: 1.5; 5; 15 mg/kg
Administration: p.o.; BID for 2 weeks
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.
Clinical Trial
Molecular Weight

421.38

Formula

C20H16FN7O3
CAS No.
SMILES

N#CC1=NN2C=CC3=NC2=C1C(NC4(COC5=NC=C(C=C5[C@H]6CCON36)F)CC4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JYP0322 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JYP03222644645-39-4ROS1-IN-3JYP 0322JYP-0322ROS KinaseTrk ReceptorTropomyosin related kinase receptorROS1;CNS-penetrant;ROS1G2032R;NSCLCInhibitorinhibitorinhibit

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