A potent inhibitor of VEGF receptors

AAL-993 – 5 mg

Brand:
Cayman
CAS:
269390-77-4
Storage:
-20
UN-No:
Non-Hazardous - /

AAL-993 is a potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively.{26698,26700} It less potently inhibits c-Kit, colony stimulating factor 1 receptor, PGDF receptor β, and EGF receptor (IC50s = 236, 380, 640, and 1,040 nM, respectively) and is without effect on a number of other tyrosine kinases.{26698} AAL-993 is orally bioavailable in vivo, blocks VEGF-induced angiogenesis, and prevents the growth of primary tumors and spontaneous peripheral metastases in mice.{26698,26699} It also inhibits hypoxia-mediated increase in hypoxia-inducible factor-1 transcriptional activity in an ERK-dependent manner (IC50 = ~5 µM).{26701}  

 

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Description

A potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively; orally bioavailable in vivo, blocking VEGF-induced angiogenesis and preventing the growth of primary tumors and spontaneous peripheral metastases in mice

Formal name: 2-​[(4-​pyridinylmethyl)​amino]​-​N-​[3-​(trifluoromethyl)​phenyl]​-benzamide

Synonyms:  VEGFR Tyrosine Kinase Inhibitor VI|ZK 260253

Molecular weight: 371.4

CAS: 269390-77-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Transcription Factors|HIF-1α||Research Area|Cancer|Tumor Microenvironment

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