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AAL-993

AAL-993 is a potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively.<sup class="referenceList">[1],[2]</sup> 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.<sup class="referenceList">[1]</sup> AAL-993 is orally bioavailable in vivo, blocks VEGF-induced angiogenesis, and prevents the growth of primary tumors and spontaneous peripheral metastases in mice.<sup class="referenceList">[1],[3]</sup> It also inhibits hypoxia-mediated increase in hypoxia-inducible factor-1 transcriptional activity in an ERK-dependent manner (IC50 = ~5 µM).<sup class="referenceList">[4]</sup>
269390-77-4
Item No.
TX007NJL
CAS No.
269390-77-4
Molecular Formula
C20H16F3N3O
Molecular Weight
371.3557
Pricing ＆ Availability
Pack Size Purity Price(USD) Availability Quantity
1mg 95% $29.00 in stock
5mg 95% $67.00 in stock
10mg 95% $111.00 in stock
25mg 95% $217.00 in stock
50mg 95% $342.00 in stock
100mg 95% $504.00 in stock
WARNING This product is for research use only. SDS
Technical Information
Item No.:
TX007NJL
Product Name:
AAL-993
Description:
Synonyms:
VEGFR Tyrosine Kinase Inhibitor VI; ZK 260253; AAL-993; AAL993
CAS Number:
269390-77-4
MDL:
MFCD18251410
Molecular Formula:
C20H16F3N3O
Molecular Weight:
371.3557
SMILES:
O=C(NC1=CC=CC(C(F)(F)F)=C1)C2=CC=CC=C2NCC3=CC=NC=C3
λmax:
220, 256, 348 nm
IC₅₀ & Target:
VEGFR1 VEGFR2 VEGFR3
130 nM (IC50) 23 nM (IC50) 18 nM (IC50)
Solubility:
DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 1 mg/ml
Shipping Condition:
Room temperature in continental US; may vary elsewhere.
References & Citations:
[1]. 1.Manley, P.W., Furet, P., Bold, G., et al. Anthranilic acid amides: A novel class of antiangiogenic VEGF receptor kinase inhibitors J. Med. Chem. 45(26),5687-5693 (2002).
[2]. Manley, P.W., Bold, G., Brüggen, J., et al. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis Biochim. Biophys. Acta 1697(1-2),17-27 (2004).
[3]. Honda, T., Tajima, H., Kaneko, Y., et al. Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity Bioorg. Med. Chem. Lett. 18(9),2939-2943 (2008).
[4]. Ban, H.S., Uno, M., and Nakamura, H. Suppression of hypoxia-induced HIF-1α accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633 Cancer Lett. 296(1),17-26 (2010).