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Chemical Structure| 1260533-36-5 Chemical Structure| 1260533-36-5

Structure of Pimitespib
CAS No.: 1260533-36-5

Chemical Structure| 1260533-36-5

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TAS-116 is a potent and selective HSP90α/β inhibitor with Kis of 34.7 nM, 21.3 nM, respectively.

Synonyms: Tas-116

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Product Details of Pimitespib

CAS No. :1260533-36-5
Formula : C25H26N8O
M.W : 454.53
SMILES Code : O=C(N)C1=CC=C(N2N=C(C(C)C)C3=C(N4C=C(C5=CN(C)N=C5)N=C4)C=CN=C32)C(CC)=C1
Synonyms :
Tas-116
MDL No. :MFCD28502196

Safety of Pimitespib

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

Related Pathways of Pimitespib

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Ba/F3-insSVD-C797S cells 1 μM 24 hours Induced apoptosis, decreased EGFR and AKT levels, induced PARP cleavage and Bim stabilization PMC10006853
Primary ATL cells 0.2-0.5 μM 72 hours Evaluate the growth inhibitory effect of TAS-116 on primary ATL cells, IC50 values ranging from 0.2 to 0.5 μmol/L PMC8819293
Su9T01 0.5 μM 72 hours Evaluate the growth inhibitory effect of TAS-116 on ATL-related cell lines, IC50 values below 0.5 μmol/L PMC8819293
ED-40515 0.5 μM 72 hours Evaluate the growth inhibitory effect of TAS-116 on ATL-related cell lines, IC50 values below 0.5 μmol/L PMC8819293
OATL4 0.5 μM 72 hours Evaluate the growth inhibitory effect of TAS-116 on ATL-related cell lines, IC50 values below 0.5 μmol/L PMC8819293
HuT-102 0.5 μM 72 hours Evaluate the growth inhibitory effect of TAS-116 on ATL-related cell lines, IC50 values below 0.5 μmol/L PMC8819293

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
CB17-SCID mice HuT-102 or Su9T01 cell xenograft model Oral 10 or 14 mg/kg Once daily for 28 days Evaluate the growth inhibitory effect of TAS-116 on xenografted ATL cells, significantly reduced tumor volume PMC8819293
Athymic nude mice (BALB/cAJcl-Foxn1nu) Ba/F3-insSVD-C797S tumor model Oral 14 mg/kg Once daily for 2 weeks Inhibited tumor growth and prolonged survival PMC10006853

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02965885 Advanced Solid Tumors Phase 1 Recruiting March 2020 United States, Ohio ... More >> Gabrail Cancer Center Recruiting Canton, Ohio, United States, 44718 University Hospitals Case Medical Center Recruiting Cleveland, Ohio, United States, 44106 United States, South Carolina Greenville Health System, Institute for Translational Oncology Research Recruiting Greenville, South Carolina, United States, 29605 United States, Virginia US Oncology - Virginia Cancer Specialists, P.C. Recruiting Fairfax, Virginia, United States, 86885 Italy Policlinico S.Orsola-Malpighi, U.O. Oncologia Medica Recruiting Bologna, Italy, 40138 Contact: Stefania Salvagni    0039 0512142204    stefania.salvagni@aosp.bo.it    Azienda Ospedaliero-Universitaria Policlinico-Vittorio Emanuele Oncologia Medica Recruiting Catania, Italy, 95123 Contact: Soto Parra    0039 0953782426    hsotoparra@policlinico.unict.it    Contact       hsotoparra@yahoo.it    Istituto Europeo di Oncologia , Sviluppo di Nuovi Farmaci per Terapie Innovative Recruiting Milano, Italy, 20141 Contact: Giuseppe Curigliano    0039 0257489439    giuseppe.curigliano@ieo.it    Regina Elena National Cancer Institute Not yet recruiting Roma, Italy, 00144 Contact: Francesco Cognetti    0039 0652666919    francesco.cognetti@ifo.gov.it    United Kingdom Northern Centre for Cancer Care Recruiting Newcastle Upon Tyne, England, United Kingdom Contact: Ruth Plummer    +44 (0) 191 208 4414    Ruth.Plummer@newcastle.ac.uk    Division of Cancer Studies, Kings College London Recruiting London, United Kingdom, SE19 9RT Sarah Cannon Research Institute UK Recruiting London, United Kingdom, W1G 6AD The Christie NHS Foundation Trust Institute of Cancer Sciences, University of Manchester Recruiting Manchester, United Kingdom, M20 4BX Royal Marsden Recruiting Sutton, United Kingdom, SM2 5PTT Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

22.00mL

4.40mL

2.20mL

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
 

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