AAL-993 | 2740

AAL-993 is a potent, selective and cell-permeable inhibitor of VEGFR-1 (IC₅₀ = 130 nM), VEGFR-2 (IC₅₀ = 23 nM) and VEGFR-3 (IC₅₀ = 18nM). At higher concentrations it inhibits PDGFR (640 nM), c-Kit (236 nM) and CSF-1R (380 nM). Inactive at other kinases such as EGFR, FGFR-1, CDK-1, Tie-2, c-Met, IGF-1R, c-Src and c-Abl. X-ray crystal studies on AAL-993 complexed to the catalytic domain of diphosphorylated VEGFR- 2 indicates that it binds to an inactive conformation of the protein. AAL-993 inhibits VEGF-induced angiogenesis (mouse model).

AAL-993 is a potent, selective and cell-permeable inhibitor of VEGFR-1 (IC₅₀ = 130 nM), VEGFR-2 (IC₅₀ = 23 nM) and VEGFR-3 (IC₅₀ = 18nM). At higher concentrations it inhibits PDGFR (640 nM), c-Kit (236 nM) and CSF-1R (380 nM). Inactive at other kinases such as EGFR, FGFR-1, CDK-1, Tie-2, c-Met, IGF-1R, c-Src and c-Abl. X-ray crystal studies on AAL-993 complexed to the catalytic domain of diphosphorylated VEGFR- 2 indicates that it binds to an inactive conformation of the protein.

2740 | AAL-993 DataSheet

Alternate Name/Synonyms: 2-((4-Pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide

Appearance: Light yellow solid

Formulation: N/A

CAS Number: 269390-77-4

Structure Available?: Y

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₀H₁₆F₃N₃O

Molecular Weight: 371.36

Cell-Permeable?: Yes

Purity: ≥98% by TLC

Solubilities: DMSO (>25 mg/ml) or EtOH (~15 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent VEGFR inhibitor

MDL Number: N/A

PubChem CID: 6398883

SMILES: C1=CC=C(C(=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NCC3=CC=NC=C3

InChi: InChI=1S/C20H16F3N3O/c21-20(22,23)15-4-3-5-16(12-15)26-19(27)17-6-1-2-7-18(17)25-13-14-8-10-24-11-9-14/h1-12,25H,13H2,(H,26,27)

InChi Key: BLAFVGLBBOPRLP-UHFFFAOYSA-N