AAL-993
- Product Name
- AAL-993
- CAS No.
- 269390-77-4
- Chemical Name
- AAL-993
- Synonyms
- CS-2315;AAL-993;AAL 993, VEGFR inhibitor;2-(Pyridin-4-ylmethylamino)-N-[3-(trifluoromethyl)phenyl]benzamide;2-[(4-Pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]benzami de;Benzamide, 2-[(4-pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]-;VEGFR Tyrosine Kinase Inhibitor VI, AAL-993 - CAS 269390-77-4 - Calbiochem;antiangiogenic,antitumor properties,AAL 993,VEGFR1,VEGFR2,orally active,VEGFR,AAL993,VEGFR3,Inhibitor,VEGFR inhibitor,AAL-993,Vascular endothelial growth factor receptor,inhibit
- CBNumber
- CB13070432
- Molecular Formula
- C20H16F3N3O
- Formula Weight
- 371.36
- MOL File
- 269390-77-4.mol
AAL-993 Property
- Melting point:
- 158-160 °C
- Boiling point:
- 441.3±45.0 °C(Predicted)
- Density
- 1.349±0.06 g/cm3(Predicted)
- storage temp.
- +2C to +8C
- solubility
- Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 15 mg/ml).
- form
- Off-white powder
- pka
- 12.95±0.70(Predicted)
- color
- Pale yellow
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
N-Bromosuccinimide Price
- Product number
- 676504
- Product name
- VEGFR Tyrosine Kinase Inhibitor VI, AAL-993 - CAS 269390-77-4 - Calbiochem
- Packaging
- 10mg
- Price
- $201
- Updated
- 2024/03/01
- Product number
- 16351
- Product name
- AAL-993
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 16351
- Product name
- AAL-993
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $128
- Updated
- 2024/03/01
- Product number
- A104490
- Product name
- AAL-993
- Packaging
- 100mg
- Price
- $1450
- Updated
- 2021/12/16
- Product number
- C3730
- Product name
- AAL-993
- Packaging
- 5mg
- Price
- $143
- Updated
- 2021/12/16
AAL-993 Chemical Properties,Usage,Production
Description
AAL-993 (269390-77-4) inhibits VEGFR-1 (IC50 = 130 nM), VEGFR-2 (IC50 = 23 nM), and VEGFR-3 (IC50 = 18 nM). PDGFR-β, cKit, and CSF-1R are also inhibited at higher concentrations (IC50‘s 640 nM, 236 nM and 380 nM respectively). Screening studies have shown no inhibitory activity against a range of other kinases. X-Ray crystallography has shown that AAL-993 binds to the catalytic domain of VEGFR-2 when the protein is in an inactive conformation. Cell permeable, active in vivo and in whole animal studies.
Uses
AAL-993 is a VEGFR tyrosine kinase inhibitor that possess dual inhibition of VEGFR signaling and HIF-1α expression through ERK inhibition without affecting Akt phosphorylation.
General Description
A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC50 = 130, 23, and 18 nM against VEGFR-1, -2, and -3, respectively; IC50 = 1.24 nM against VEGF-induced human VEGFR-2 phosphorylation in CHO cells) by targeting the ATP-binding site of VEGFR in its inactive "DFG-out" conformation and effectively suppresses tumor growths (50 to 100 mg/kg; p.o.) via its anti-angiogenesis activity in mice and rats in vivo, while inhibiting c-kit, CSF-1R/c-Fms, PDGFR-β, and c-Abl only at higher concentrations (IC50 = 236, 380, 640, and 2820 nM, respectively). AAL933 and two other VEGFR inhibitors, KRN633 and SU5416, are also shown to inhibit hypoxia-induced HIF-1α expression (by <90% at 30 M) and transcription activation. Unlike KRN633 and SU5416, AAL933 prevents only hypoxia-induced Erk, but not Akt, phosphorylation in HeLa cells.
in vitro
aal-993 was found to be a highly potent and selective inhibitor of the recombinant vegfr-2 and vegfr-3 kinases. at 3- to 5-fold higher concentration, aal-993 also inhibited vegfr-1 and, although it possessed some activity against other members of the pdgfr kinase family at submicromolar concentrations, aal-993 did not significantly inhibit any of the other kinases tested at concentrations
in vivo
animal efficacy study found that aal-993 was able to potently inhibit vegf-induced angiogenesis in an implant model, with ed50 values of 7 mg/kg. moreover, in a mouse orthotopic model of melanoma, aal-993 could potently inhibit both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases [1].
IC 50
130, 23, and 18 nm for vegfr1, 2, and 3, respectively
References
1) Manley et al. (2002), Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors; J. Med. Chem., 45 5687 2) Manley et al. (2004), Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis; Biochim. Biophys. Acta, 1697 17
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