Synonyms: PR610 | tarloxotinib cation | TH-4000
Compound class:
Synthetic organic
Comment: Tarloxotinib (TH-4000) is a hypoxia-activated prodrug (HAP) [1] being developed by Threshold Pharmaceuticals. Delivered as the bromide salt (PubChem CID 51038315) as described in its INN record. The compound undergoes activation selectively within the hypoxic tumour compartment to produce an irreversible pan-ErbB tyrosine-kinase inhibitor, represented by TH-4000E [1]. The 4-nitroimidazole trigger on the tertiary amine side chain facilitates activation. This is one of the first molecularly targeted HAPs to be developed.
|
|
Classification | |
Compound class | Synthetic organic |
Is prodrug? | Yes |
Active form | TH-4000E |
IUPAC Name |
[(E)-4-[[4-(3-bromo-4-chloroanilino)pyrido[3,4-d]pyrimidin-6-yl]amino]-4-oxobut-2-enyl]-dimethyl-[(3-methyl-5-nitroimidazol-4-yl)methyl]azanium |
International Nonproprietary Names | |
INN number | INN |
10229 | tarloxotinib bromide |
Synonyms |
PR610 | tarloxotinib cation | TH-4000 |
Database Links | |
CAS Registry No. | 1636938-13-0 (source: SciFinder) |
GtoPdb PubChem SID | 328083511 |
PubChem CID | 51038316 |
Search Google for chemical match using the InChIKey | MUJMYVFVAWFUJL-SNAWJCMRSA-O |
Search Google for chemicals with the same backbone | MUJMYVFVAWFUJL |
Search PubMed clinical trials | tarloxotinib bromide |
Search PubMed titles | tarloxotinib bromide |
Search PubMed titles/abstracts | tarloxotinib bromide |
UniChem Compound Search for chemical match using the InChIKey | MUJMYVFVAWFUJL-SNAWJCMRSA-O |
UniChem Connectivity Search for chemical match using the InChIKey | MUJMYVFVAWFUJL-SNAWJCMRSA-O |