AM555S,TAC-101
AM555S,TAC-101 Basic information
- Product Name:
- AM555S,TAC-101
- Synonyms:
-
- AM555S,TAC-101
- AM 555S
- AMsilarotene
- AMsilarotene (TAC-101)
- 4-[[3,5-Bis(trimethylsilyl)benzoyl]amino]benzoic acid
- CS-893
- 4-(3,5-bis(trimethylsilyl)benzamido)benzoic acid
- Benzoic acid,4-[[3,5-bis(trimethylsilyl)benzoyl]amino]-
- CAS:
- 125973-56-0
- MF:
- C20H27NO3Si2
- MW:
- 385.6
- Mol File:
- 125973-56-0.mol
AM555S,TAC-101 Chemical Properties
- Melting point:
- 280℃ (decomposition)
- Boiling point:
- 403.3±45.0 °C(Predicted)
- Density
- 1.10±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 100 mg/mL (259.34 mM; Need ultrasonic)
- form
- Solid
- pka
- 4.28±0.10(Predicted)
- color
- White to off-white
AM555S,TAC-101 Usage And Synthesis
Uses
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer[1][2][3].
in vivo
Amsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice[2].
| Animal Model: | 6-week-old female BALB/c nu/nu mice with subcutaneous RMG-II tumors[2] |
| Dosage: | 8 mg/kg/day |
| Administration: | Orally for 30 days |
| Result: | The maximal tumor growth-inhibiting effect was seen on day 31 of administration, when there was a 45% reduction of relative tumor volume (RTV). |
References
[1] Sun SY, et al. Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells. Cancer Res. 1997 Nov 1;57(21):4931-9. PMID:9354460
[2] Suzuki N, et al. A novel retinoid, 4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid (TAC-101), induces apoptosis of human ovarian carcinoma cells and shows potential as a new antitumor agent for clear cell adenocarcinoma. Gynecol Oncol. 2004 Sep;94(3):643-9. DOI:10.1016/j.ygyno.2004.06.026
[3] Fujimoto K, et al. Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44. DOI:10.1002/(sici)1097-0215(19990517)81:43.0.co;2-4
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