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Cat. No. Name Size Price Add Cart
KI0821ABR-215050QuoteQuote

Chemical Characteristic

Product NameABR-215050
SynonymsTasquinimod, TasQ
CAS No.254964-60-8
Molecular Weight 406.36
FormulaC20H17F3N2O4
Chemical Structure

Biological activities

ABR-215050 is a quinoline-3-carboxamide anti-angiogenic agent. ABR-215050 is an allosteric modulator of HDAC4 survival signaling. The IC50 of ABR-215050 is 50 nM against blocking the formation of HDAC4/N-CoR/HDAC3 complexes. ABR-215050 inhibits the binding of HDAC4 to N-CoR/HDAC3 complexes within PCs with an IC50 of less than 1 µM. ABR-215050 allosterically binds to the regulatory Zn2+ binding domain of HDAC4 with a Kd ranging from 10 to 30 nM. ABR-215050 inhibits growth of human PC cells (LNCaP, LAPC-4, and CWR-22Rv1) and HUVECs. ABR-215050 suppresses hypoxia-induced decrease in histone acetylation without lowering HDAC expression or directly inhibiting HDAC activity.[1] ABR-215050 selectively decreases tumor oxygen content by inhibiting tumor angiogenesis. ABR-215050 given orally in the drinking water at a dose of 10mg/kg body weight/day maintains the serum ABR-215050 in adult male nude mice at 0.5閳?µM.[2] ABR-215050 profoundly inhibits tumor growth in nude mice bearing CWR-22RH human prostate tumors.[3]

Protocols

In vitro: For the determination of clonogenic survival fraction of HUVECs, DMECs, and CWR22Rv1 cells to radiation alone and in combination with ABR-215050 , these cells are washed with phosphate buffered saline (PBS), trypsinized, and the number of single cells counted using an Auto T4 Nexcelom Cellometer. The single cell suspensions are then plated in triplicate at 500閳?000 cells/60 mm tissue culture dish and the next day the cultures irradiated with 0, 2, 4, or 6 Gy using a 137Cs AECL Gamma cell 40 閳ユ悆rradiator at appropriately 1 Gy/minute. The media is then change to media containing 0, 1, or 10 µM ABR-215050. The cultures are then allowed 10閳?4 days before the medium is removed and the dishes washed twice with PBS and 2 mL of 0.5% crystal violet staining solution in 25% methanol added to each dish for 1閳? minutes, followed by wash out with water. The dishes are air dried and the number of surviving colonies counted with a stereo-microscope. The clonogenic survival fraction is determined by dividing the number of colonies per dish by the number of cells seeded. For comparison, these clonogenic survival fractions for the various treatments are normalized by dividing these values by the mean clonogenic survival fraction for the untreated non-irradiated cells.[2] In vivo: Nude BALB/c mice are used for subcutaneous implantation of human prostate tumor cells LNCaP and CWR-22RH. Tumor growth is measured with a microcaliper twice a week throughout the experiment, and the final tumor burden is measured by weight on the day of termination of the experiment. Distribution of ABR-215050 at 1 mg/kg/day and 10 mg/kg/day (administered orally via the drinking water) started on day 7 after inoculation.[3]

References

[1] Isaacs JT, et al. Tasquinimod is an allosteric modulator of HDAC4 survival signaling within the compromised cancer microenvironment. Cancer Res. 2013, 73(4): 1386-1399. 閵嗏偓閵嗏偓
[2] Dalrymple SL, et al. Tasquinimod prevents the angiogenic rebound induced by fractionated radiation resulting in an enhanced therapeutic response of prostate cancer xenografts. Prostate. 2012, 72(6): 638-648. 閵嗏偓閵嗏偓
[3] Olsson A, et al.Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors. Mol Cancer. 2010, 9:107. 閵嗏偓閵嗏偓

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