| Bioactivity | 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]. |
| Invitro | 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]. |
| Name | AAL993 |
| CAS | 269390-77-4 |
| Formula | C20H16F3N3O |
| Molar Mass | 371.36 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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. |