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Purity: ≥98%
AAL-993 is a novel, orally bioavailable and highly potent VEGFR inhibitor that inhibits VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively. It is inactive against several other tyrosine kinases and less effective against c-Kit, colony stimulating factor 1 receptor, PGDF receptor β, and EGF receptor (IC50s = 236, 380, 640, and 1,040 nM, respectively). In mice, AAL-993 inhibits the growth of primary tumors and spontaneous peripheral metastases by blocking VEGF-induced angiogenesis. In an ERK-dependent manner, it also suppresses the increase in hypoxia-inducible factor-1 transcriptional activity (IC50 = ~5 µM).
| Targets |
VEGFR1 (IC50 = 130 nM); VEGFR2 (IC50 = 23 nM); VEGFR3 (IC50 = 18 nM)
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|---|---|
| ln Vitro |
AAL993 inhibits ERK to suppress HIF-1α expression while leaving Akt phosphorylation unaffected[2].
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| ln Vivo |
AAL993 (compound 5) has a potent inhibitory effect on VEGF-induced angiogenesis in an implant model, with an ED50 value of 7 mg/kg [1].
AAL993 (24–100 mg/kg; p.o.; daily; for 14 days) inhibits the formation of spontaneous peripheral metastases as well as the growth of the primary tumor in the B16 melanoma xenograft model[1]. |
| References |
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| Molecular Formula |
C20H16N3OF3
|
|---|---|
| Molecular Weight |
371.35574
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| Exact Mass |
371.12
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| Elemental Analysis |
C, 64.69; H, 4.34; F, 15.35; N, 11.32; O, 4.31
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| CAS # |
269390-77-4
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| Related CAS # |
269390-77-4
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C(=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NCC3=CC=NC=C3
|
| InChi Key |
BLAFVGLBBOPRLP-UHFFFAOYSA-N
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| InChi Code |
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)
|
| Chemical Name |
2-(pyridin-4-ylmethylamino)-N-[3-(trifluoromethyl)phenyl]benzamide
|
| Synonyms |
AAL 993; AA-L993; AAL993
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~125 mg/mL (~336.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6928 mL | 13.4640 mL | 26.9280 mL | |
| 5 mM | 0.5386 mL | 2.6928 mL | 5.3856 mL | |
| 10 mM | 0.2693 mL | 1.3464 mL | 2.6928 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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