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AAL993 

Cat. No. M29767
AAL993  Structure
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 371.36
Formula C20H16F3N3O
CAS Number 269390-77-4
Form Solid
Solubility (25°C) DMSO 125 mg/mL (ultrasonic)
Storage 4°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hyun Seung Ban, et al. Cancer Lett. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633

[2] Takahiro Honda, et al. Bioorg Med Chem Lett. Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity

[3] Paul William Manley, et al. Biochim Biophys Acta. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis

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  Catalog
Abmole Inhibitor Catalog




Keywords: AAL993  supplier, VEGFR/PDGFR, inhibitors, activators


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