An irreversible pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6

PF-299804 – 10 mg

Brand:
Cayman
CAS:
1110813-31-4
Storage:
-20
UN-No:
Non-Hazardous - /

The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.{17857,18353} PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors.{27742,27743} At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.{27742,27743}  

 

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SKU: 9001879 - 10 mg Category:

Description

An irreversible pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively); demonstrates antitumor activity in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors

Formal name: N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-(2E)-butenamide

Synonyms:  Dacomitinib|PF299

Molecular weight: 469.9

CAS: 1110813-31-4

Purity: ≥98%

Formulation: A crystalline solid

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