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Chemical Structure| 1802929-43-6 Chemical Structure| 1802929-43-6

Structure of PRN1371
CAS No.: 1802929-43-6

Chemical Structure| 1802929-43-6

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PRN1371 is an irreversible covalent FGFR inhibitor used for the treatment of solid tumor.

Synonyms: PRN1371

4.5 *For Research Use Only !

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Product Details of PRN1371

CAS No. :1802929-43-6
Formula : C26H30Cl2N6O4
M.W : 561.46
SMILES Code : O=C1C(C2=C(Cl)C(OC)=CC(OC)=C2Cl)=CC3=CN=C(NC)N=C3N1CCCN4CCN(C(C=C)=O)CC4
Synonyms :
PRN1371
MDL No. :MFCD31560471

Safety of PRN1371

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

Related Pathways of PRN1371

RTK

Isoform Comparison

Biological Activity

Target
  • FGFR2

    FGFR2, IC50:1.3 nM

  • FGFR3

    FGFR3, IC50:4.1 nM

  • FGFR4

    FGFR4, IC50:19.3 nM

  • FGFR1

    FGFR1, IC50:0.6 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
KAI-3 1.0 μM 2 h PRN371 inhibited the downstream effector proteins of JAK3-STAT signaling in KAI-3 cells PMC5940653
NK92 1.0 μM 2 h PRN371 inhibited the downstream effector proteins of JAK3-STAT signaling in NK92 cells PMC5940653
CMK 1.0 μM 72 h PRN371 dose-dependently suppressed the growth of CMK cells and induced apoptosis through abrogation of JAK3-STAT signaling PMC5940653
NK-S1 1.0 μM 72 h PRN371 dose-dependently suppressed the growth of NK-S1 cells and induced apoptosis through abrogation of JAK3-STAT signaling PMC5940653

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice NK-S1 subcutaneous xenograft model Intraperitoneal injection 25 or 50 mg/kg Once daily for 14 days PRN371 significantly inhibited tumor growth in the NK-S1 xenograft model without causing significant weight loss or toxicity PMC5940653

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02608125 Solid Tumors|Metastatic Urothe... More >>lial Carcinoma & Renal Pelvis & Ureter Less << PHASE1 TERMINATED 2020-06-23 UCSF Helen Diller Family Compr... More >>ehensive Cancer Cener, San Francisco, California, 94115, United States|Johns Hopkins Medicine, Baltimore, Maryland, 21205, United States|Wake Forest University Health Sciences Medical Center, Winston-Salem, North Carolina, 27157, United States|Tennessee Oncology, Sarah Canon Research Institute, Nashville, Tennessee, 37203, United States|The University of Texas MD Anderson Cancer Center, Houston, Texas, 77030, United States|Vall d'Hebron Institute of Oncology (VHIO), Vall d'Hebron University Hospital, Barcelona, 08035, Spain|Hospital General Universitario de Elche, Elche, 03203, Spain|Hospital Universitario Ramon y Cajal, Madrid, 28034, Spain|START Madrid-FJD Fundacion Jiminez Diaz, Madrid, 28040, Spain|Hospital Universitario 12 de Octubre, Madrid, 28041, Spain|START Madrid-CIOCC, Centro Integral Oncológico Clara Campal, Madrid, 28050, Spain|Hospital Virgen del Rocio, Seville, 41013, Spain Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.91mL

1.78mL

0.89mL

17.81mL

3.56mL

1.78mL

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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