tasquinimod
- CAS No.254964-60-8
- Chemical Name:tasquinimod
- CBNumber:CB61508619
- Molecular Formula:C20H17F3N2O4
- Formula Weight:406.36
- MOL File:254964-60-8.mol
- Boiling point 501.5±50.0 °C(Predicted)
- Density 1.427±0.06 g/cm3(Predicted)
- storage temp. 2-8°C
- solubility insoluble in H2O; ≥20.32 mg/mL in DMSO; ≥4.75 mg/mL in EtOH with gentle warming and ultrasonic
- form solid
- pka 4.50±1.00(Predicted)
- color White to light yellow
- FDA UNII 756U07KN1R
- NCI Drug Dictionary tasquinimod
- UNSPSC Code 12352200
- NACRES NA.77
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H315-H319-H335
- Precautionary statements P261-P305+P351+P338
tasquinimod Chemical Properties,Usage,Production
-
Description
Tasquinimod is an orally-active quinoline-
3- carboxamide derived from roquinimex, an immunomodulatory quinolone with applications in some cancers and autoimmune diseases. Tasquinimod inhibits tumor angiogenesis and supplements radiation or chemotherapy in animal models of prostate cancer. While its precise mechanism of action remains unclear, tasquinimod has been reported to alter signaling through S100A9, thrombospondin-1, HIF-1α, androgen receptor, VEGF, and HDAC3/4. - Uses Tasquinimod is an orally active antiangiogenic agent which may inhibit HDAC4 signalling. This affects cancer cell survival thus making this compound and anti-cancer agent.
-
in vivo
The bioavailability and oral absorption of Tasquinimod is excellent when adult male mice (i.e., C57Bl/6J, or athymic nude mice) are given 0.1-30 mg/kg (i.e., 0.2-74 μmoles/kg) via gavage or the drinking water. The potency of Tasquinimod expressed as the daily oral dose of Tasquinimod which inhibits cancer growth by 50% ranges from 0.1-1.0 mg/kg/d (i.e., 0.24-2.40 μmoles/kg/day) against a series (n>5) of human prostate cancer xenografts in immune-deficient mice. Tasquinimod at a chronic dose of 5 mg/kg/day via the drinking water produces > 80% inhibition (p<0.05) of TRAMP-C2 mouse prostate cancer growth in immune-competent syngeneic mice[2]. Nude mice carrying subcutaneous LNCaP tumors are treated with Tasquinimod for 3 weeks. Exposure to Tasquinimod at 1 mg/kg/day and 10 mg/kg/day started on day 7 after inoculation. There is a statistically significant dose dependent reduction in tumor weight both at 1 mg/kg/day and 10 mg/kg/day compare to the untreated control group 28 days after inoculation (p<0.001), illustrating the anti-tumor effect of Tasquinimod[3].
- target tumor microenvironment
- IC 50 HDAC4: 10-30 nM (Kd)
- storage Store at -20°C
-
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- Inhibitors
- S100 calcium binding protein A9 modulator
- Angiogenesis inhibitor
- 抑制剂
- 合成有机化合物配体
- 标准品
- 细胞周期
- 小分子抑制剂,天然产物
- 他喹莫德,10 MM DMSO 溶液
- 他喹莫德|||ABR-215050
- 他喹莫德 3级
- 4-羟基-5-甲氧基-N,1-二甲基-2-氧代-N-(4-(三氟甲基)苯基)-1,2-二氢喹啉-3-甲酰胺
- 他喹莫德, >98%
- 他喹莫德
- 254964-60-8
- Tasquinimod, 10 mM in DMSO
- 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]quinoline-3-carboxamide
- 4-Hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-(4-(trifluoromethyl)phenyl)-1,2-dihydroquinoline-3-carboxamide
- 7-Dimethoxy-quinolin-4-yloxy)-phenylamine
- 7-diMethoxy-4-quinolinyl)oxy]-
- TASQ)
- Tasquinimod(ABR-215050)
- Tasquinimod, >98%
- ABR-215050; ABR215050; ABR 215050
- 4-Hydroxy-N-[4-(trifluoromethyl)phenyl]-5-methoxy-N,1-dimethyl-2-oxo-1,2-dihydroquinoline-3-carboxamide
- 4-Hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-(4-(trifluoromethyl)-phenyl)-1,2-dihydroquinoline-3-c
- 1,2-dihydro-4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-trifluoromethyl)phenyl]-3-quinolinecarboxamide
- 4-Hydroxy-5-Methoxy-1-Methyl-2-oxo-1,2- dihydro-quinoline-3-carboxylic acid Methyl- (4-trifluoroMethyl-phenyl)-aMide
- 3-QuinolinecarboxaMide, 1,2-dihydro-4-hydroxy-5-Methoxy-N,1-diMethyl-2-oxo-N-[4-(trifluoroMethyl)phenyl]-
- ABR-215050
- tasquinimod
- N-Methyl-N-(4-trifluoromethylphenyl)-1,2-dihydro-4-hydroxy-5-methoxy-1-methyl-2-oxoquinoline-3-carboxamide
- 4-Hydroxy-5-methoxy-N-methyl-1-methyl-2-oxo-N-(4-trifluoromethylphenyl)-1,2-dihydroquinoline-3-carboxamide