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Tarloxotinib bromide Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5754010

MBS5754010 is an inhibitor targeting Tarloxotinib bromide. Tarloxotinib bromide is an irreversible inhibitor of EGFR/HER2. More details

Product Documentation
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Sample Manual Insert View PDF
PDF
Testing Data View PDF
PDF
Certificate of Analysis (COA) View PDF
PDF
QC Report View PDF
PDF
Material Safety Data Sheet View PDF
PDF
Technical Datasheet View PDF
PDF
Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Tarloxotinib bromide, Inhibitor
Full Product Name
Tarloxotinib bromide
Product Synonym Names
TH-4000
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
681.77
Solubility
DMSO: 33mg/mL (48.40mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C24H24Br2ClN9O3
SMILES
BrC1=C(Cl)C=CC(NC2=NC=NC3=C2C=C(NC(/C=C/C[N+](C)(C)CC4=C([N+]([O-])=O)N=CN4C)=O)N=C3)=C1.[Br-]
CAS Number
1636180-98-7
Target & IC50
EGFR/HER2
In Vitro
The prototype WT EGFR-driven xenograft model (A431) was used to "reverse" the plasma exposure of each drug in human subjects reported back to the xenograft model, so that the baseline tallotinib bromide for each EGFR-TKI Activity. Only treatment with clinically relevant doses and schedules of Tarloxotinib bromide is associated with tumor regression and durable inhibition of WT EGFR tumor phosphorylation.Consistent with these findings, tarotinib bromide treatment, can also return the WT EGFR NSCLC tumor models H125 and H1648, proving that tarotinib bromide provides the necessary therapeutic indicators for inhibiting WT EGFR in vivo[1].

Product References and Citations for Tarloxotinib bromide, inhibitor

Shevan Silva, Abstract A67: Preclinical efficacy of tarloxotinib bromide (TH-4000), a hypoxia-activated EGFR/HER2 inhibitor: rationale for clinical evaluation in EGFR mutant, T790M-negative NSCLC following progression on EGFR-TKI therapy. Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston, MA.
Shevan Silva, Abstract A67: Preclinical efficacy of tarloxotinib bromide (TH-4000), a hypoxia-activated EGFR/HER2 inhibitor: rationale for clinical evaluation in EGFR mutant, T790M-negative NSCLC following progression on EGFR-TKI therapy. Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston, MA.
Adam V. Patterson, Abstract 5358: The hypoxia-activated EGFR-TKI TH-4000 overcomes erlotinib-resistance in preclinical NSCLC models at plasma levels achieved in a Phase 1 clinical trial. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.
Adam V. Patterson, Abstract 5358: The hypoxia-activated EGFR-TKI TH-4000 overcomes erlotinib-resistance in preclinical NSCLC models at plasma levels achieved in a Phase 1 clinical trial. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

Other Notes

Small volumes of Tarloxotinib bromide, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.
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