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Chemical Structure| 332012-40-5 Chemical Structure| 332012-40-5

Structure of Telatinib
CAS No.: 332012-40-5

Chemical Structure| 332012-40-5

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Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.

Synonyms: Bay 57-9352

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Product Details of Telatinib

CAS No. :332012-40-5
Formula : C20H16ClN5O3
M.W : 409.83
SMILES Code : O=C(C1=CC(COC2=NN=C(C3=C2OC=C3)NC4=CC=C(C=C4)Cl)=CC=N1)NC
Synonyms :
Bay 57-9352
MDL No. :MFCD18251453

Safety of Telatinib

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

Related Pathways of Telatinib

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR3

    VEGFR3, IC50:4 nM

  • VEGFR2

    VEGFR2, IC50:6 nM

  • PDGFRα

    PDGFRα, IC50:15 nM

  • c-Kit

    c-Kit, IC50:1 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
H460/MX20 1 μM 72 hours After 72 hours of treatment with Telatinib, no significant changes in the expression and localization of ABCG2 were observed in H460/MX20 cells. PMC3983711
ABCG2-482-R2 1 μM 240 minutes To determine the effect of VKJP1 and VKJP3 on intracellular accumulation of [3H]-mitoxantrone. Results showed that VKJP1 and VKJP3 significantly increased the intracellular accumulation of [3H]-mitoxantrone in ABCG2-482-R2 cells. PMC3983711
HEK293/pcDNA3.1 1 μM 2 hours To evaluate the effect of VKJP1 and VKJP3 on ABCG2 expression. Results showed that the protein levels of ABCG2 were not significantly altered by VKJP1 or VKJP3 treatment for up to 72 h. PMC3983711
DBTRG cells 1 μM Evaluate the inhibitory effect of CPI-455 on DBTRG cell proliferation, showing no significant difference in sensitivity between WT and TMZ-resistant cells PMC3053964
MDCK cells 1 μM Evaluate the inhibitory effect of GA-A on cyst growth in MDCK cells, showing significant inhibition without cytotoxicity. PMC3053964
IPSC-ECSERPINE1-FOSB 5 µM 14 hours To investigate the effect of Telatinib on the expression of FOSB, SERPINE1, and SERPINE1-FOSB fusion transcript in iPSC-ECSERPINE1-FOSB cells. Results showed that when normalized to RPL36AL and TMBIM6, SERPINE1-FOSB expression was reduced in telatinib-treated iPSC-ECSERPINE1-FOSB cells. PMC9519970
ABCG2-overexpressing cells 0.25, 0.5, 1 μM Telatinib significantly reversed ABCG2-mediated multidrug resistance, enhancing the sensitivity to chemotherapeutic agents PMC4276951

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice ABCG2-overexpressing H460/MX20 tumor xenograft model Oral 15 mg/kg Every 2-3 days, total 12 times Telatinib in combination with doxorubicin significantly reduced the growth rate and tumor size of ABCG2-overexpressing H460/MX20 tumors, indicating that Telatinib can reverse ABCG2-mediated multidrug resistance in vivo. PMC3983711
Nude mice ABCG2-overexpressing tumor model 15 mg/kg Combination of telatinib with doxorubicin significantly reduced the growth rate and size of ABCG2-overexpressing tumors PMC4276951

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00952497 Gastric Cancer Phase 2 Completed - United States, California ... More >> UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 United States, Georgia Central Georgia Cancer Care, P.C. Macon, Georgia, United States, 31201 United States, Pennsylvania University of Pennsylvania, Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Tennessee The West Clinic Memphis, Tennessee, United States, 38120 United States, Texas The University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Spain Hospital Vall d' Hebron Barcelona, Spain, 08035 Hospital Universitari Germans Trias i Pujol Barcelona, Spain, 08916 Hospital Universitario Ramon y Cajal Madrid, Spain, 28034 Hospital Clinico San Carlos Madrid, Spain, 28040 Hospital Universitario 12 de Octubre Madrid, Spain, 28041 Hospital Universitario Marques de Valdecilla Santander, Spain, 39008 Less <<
NCT03175497 Solid Tumor, Adult Phase 1 Recruiting June 1, 2018 China ... More >> Fudan University, Zhongshan Hospital Recruiting Shanghai, China Contact: Taishu Liu Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.20mL

2.44mL

1.22mL

24.40mL

4.88mL

2.44mL

References

 

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