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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
DBTRG cells 1 μM GA-coupled beads precipitated HSP90 and VDAC, and treatment with 17AAG or GA did not affect VDAC binding. Proc Natl Acad Sci U S A. 2011 Mar 8;108(10):4105-10.
MDCK cells 1 μM GA-coupled beads precipitated HSP90 and VDAC, and treatment with 17AAG or GA did not affect VDAC binding. Proc Natl Acad Sci U S A. 2011 Mar 8;108(10):4105-10.
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. Biochem Pharmacol. 2014 May 1;89(1):52-61.
ABCG2-482-R2 1 μM 240 minutes Telatinib significantly reduced the efflux rate of [3H]-MX in ABCG2-482-R2 cells, indicating that Telatinib increases intracellular drug levels by inhibiting the drug efflux function of ABCG2. Biochem Pharmacol. 2014 May 1;89(1):52-61.
HEK293/pcDNA3.1 1 μM 2 hours Telatinib significantly increased the intracellular accumulation of [3H]-MX in ABCG2-transfected cells, suggesting that Telatinib may increase intracellular drug levels by inhibiting the drug efflux function of ABCG2. Biochem Pharmacol. 2014 May 1;89(1):52-61.
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. Sci Rep. 2022 Sep 28;12(1):16160.
ABCG2-overexpressing cells 0.25, 0.5, 1 μM Telatinib significantly reversed ABCG2-mediated multidrug resistance, enhancing the sensitivity to chemotherapeutic agents Cancers (Basel). 2014 Sep 29;6(4):1925-52.

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. Biochem Pharmacol. 2014 May 1;89(1):52-61.
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 Cancers (Basel). 2014 Sep 29;6(4):1925-52.

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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