Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

532912 CIP2A Inhibitor, TD-19 - CAS 1403933-79-8 - Calbiochem

TD-19, CIP2A inhibitor, Erlotinib analog

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N4-(3-ethynylphenyl)-6,7-dimethoxy-N2-(4-phenoxyphenyl)quinazoline-2,4-diamine, TD19

Primary Target: CIP2A
View Products on Sigmaaldrich.com
532912
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1403933-79-8C₃₀H₂₄N₄O₃

Products

Catalogue NumberPackaging Qty/Pack
5.32912.0001 玻璃瓶 10 mg
Description
OverviewA cell-permeable chemically modified derivative of erlotinib that is shown to be more effective in inducing apoptosis in H358, H441, H460, and A549 lung cancer cell lines (~10 µM). Highly effective in reducing the viability and inducing apotosis in erlotinib resistantH460 cells over-expressing CIP2A (cancerous inhibitor of protein phosphatase 2A ) that are resistant to erlotinib. Exhibits low binding affinity to the ATP binding site of the EGFR tyrosine kinase domain and has minimal effect on the phosphorylation of EGFR. Its anti-tumor effects are shown to be mediated via down-regulation of CIP2A and p-AKT expression and increased PP2A activity. Suppresses the growth of H460 xenograft tumors in NCr nude mice by approximately 80% (10 mg/kg. p.o. daily).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number532912
Brand Family Calbiochem®
SynonymsN4-(3-ethynylphenyl)-6,7-dimethoxy-N2-(4-phenoxyphenyl)quinazoline-2,4-diamine, TD19
DescriptionCIP2A Inhibitor, TD-19
References
ReferencesChao, T.T., et al. 2014. J. Pharm. Exp. Ther. 351,352.
Product Information
CAS number1403933-79-8
FormOff-white solid
Hill FormulaC₃₀H₂₄N₄O₃
Chemical formulaC₃₀H₂₄N₄O₃
Quality LevelMQ100
Applications
Biological Information
Primary TargetCIP2A
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.32912.0001 04055977281965

Documentation

CIP2A Inhibitor, TD-19 - CAS 1403933-79-8 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Chao, T.T., et al. 2014. J. Pharm. Exp. Ther. 351,352.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision09-September-2016 JSW
SynonymsN4-(3-ethynylphenyl)-6,7-dimethoxy-N2-(4-phenoxyphenyl)quinazoline-2,4-diamine, TD19
DescriptionA cell-permeable chemically modified derivative of erlotinib that is shown to be more effective in inducing apoptosis in H358, H441, H460, and A549 lung cancer cell lines (~10 µM). Highly effective in reducing the viability and inducing apotosis in erlotinib resistantH460 cells over-expressing CIP2A (cancerous inhibitor of protein phosphatase 2A ) that are resistant to erlotinib. Exhibits low binding affinity to the ATP binding site of the EGFR tyrosine kinase domain and has minimal effect on the phosphorylation of EGFR. Its anti-tumor effects are shown to be mediated via down-regulation of CIP2A and p-AKT expression and increased PP2A activity. Suppresses the growth of H460 xenograft tumors in NCr nude mice by approximately 80% (10 mg/kg. p.o. daily).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1403933-79-8
Chemical formulaC₃₀H₂₄N₄O₃
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml with warming; solution will fall out of solution at room temperature) or DMF
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesChao, T.T., et al. 2014. J. Pharm. Exp. Ther. 351,352.