269390-77-4

269390-77-4 structure

Name: AAL 993
Chemical Name: 2-[(4-Pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]benzami de
CAS Number: 269390-77-4
Molecular Formula: C₂₀H₁₆F₃N₃O
Molecular Weight: 371.356
Create Date: 2016-10-18 14:56:24
Modify Date: 2024-01-10 23:04:49
IC50s of 130 nM, 23 nM, and 18 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. AAL993 shows less potently inhibits other tyrosine kinases. AAL993 possesses potent antiangiogenic and antitumor properties[1].

Name	2-[(4-Pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]benzami de
Synonyms	2-[(pyridin-4-ylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide 2-((4-pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide 2-[(4-Pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide Benzamide, 2-[(4-pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]- AAL993

Description	IC50s of 130 nM, 23 nM, and 18 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. AAL993 shows less potently inhibits other tyrosine kinases. AAL993 possesses potent antiangiogenic and antitumor properties[1].
Related Catalog	Research Areas >> Cancer Research Areas >> Cardiovascular Disease Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR
Target	VEGFR1:130 nM (IC50) VEGFR2:23 nM (IC50) VEGFR3:18 nM (IC50)
In Vitro	AAL993 suppresses HIF-1α expression through ERK inhibition without affecting Akt phosphorylation[2].
In Vivo	AAL993 (compound 5) potently inhibits VEGF-induced angiogenesis in an implant model, with an ED50 value of 7 mg/kg[1]. In B16 melanoma xenograft model, AAL993 (24-100 mg/kg; p.o.; daily; for 14days) inhibits both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases[1].
References	[1]. Paul W Manley , et al. Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. [2]. Hyun Seung Ban, et al. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010 Oct 1;296(1):17-26.