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Amsilarotene

Catalog No. T21314 CAS 125973-56-0

Synonyms: TAC-101, TAC 101, TAC101

Amsilarotene (TAC101) inhibits the phosphorylation of retinoblastoma gene product (RB) and increases the presence of 2 cyclin-dependent kinases (CDK) inhibitors resulting in cell cycle arrest. This agent also causes a cytotoxic decline in the thymidylate synthase and cyclin A expression.

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Amsilarotene, CAS 125973-56-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 60.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 239.00
25 mg	In stock	$ 478.00
50 mg	In stock	$ 689.00
100 mg	In stock	$ 982.00
1 mL * 10 mM (in DMSO)	In stock	$ 162.00

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Purity: 99.27%

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Description	Amsilarotene (TAC101) inhibits the phosphorylation of retinoblastoma gene product (RB) and increases the presence of 2 cyclin-dependent kinases (CDK) inhibitors resulting in cell cycle arrest. This agent also causes a cytotoxic decline in the thymidylate synthase and cyclin A expression.
Targets&IC50	RARβ:400 nM (Ki), RARα:2.4 nM (Ki)
In vitro	Preclinical models have shown that Amsilarotene(4-[3,5-bis(trimethylsilyl) benzamide] benzoic acid), an oral synthetic retinoid, has antitumor activity in hepatocellular carcinoma (HCC).
In vivo	We conducted a phase I study in Japanese patients with advanced HCC to examine the pharmacokinetics, recommended dose, safety, and efficacy of Amsilarotene. The administered dose of Amsilarotene was 10 mg/day in four patients (level 1), 20 mg/day in six (level 2), and 30 mg/day in three (level 3). There was no dose-limiting toxicity at level 1. Only one patient each had dose-limiting toxicity at level 2 (grade 2 fatigue, recovery requiring eight or more consecutive days of rest) and at level 3 (grade 3 splenic vein thrombosis). Level 3 (30 mg/day) was considered the maximum tolerated dose and 20 mg/day the recommended dose by a panel of medical experts, placing maximum emphasis on safety. The most frequent adverse events were fatigue, headache, and dermal symptoms such as rash. Pharmacokinetic parameters in Japanese patients with HCC were similar to those in patients in the United States, most of whom were Caucasian. Although no patient had a complete or partial response, the disease control rate was 38.5%. In conclusion, the recommended dose of Amsilarotene for patients with HCC is 20 mg/day. Amsilarotene had an acceptable toxicity profile, warranting further evaluation in clinical trials.

Synonyms	TAC-101, TAC 101, TAC101
Molecular Weight	385.6
Formula	C20H27NO3Si2
CAS No.	125973-56-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/ml (155.6 mM)

H2O: Insoluble

References and Literature

1. Okusaka T, Ueno H, Ikeda M, Takezako Y, Morizane C. Phase I study of TAC-101, an oral synthetic retinoid, in Japanese patients with advanced hepatocellular carcinoma. Cancer Sci. 2012 Aug;103(8):1524-30. doi: 10.1111/j.1349-7006.2012.02334.x. Epub 2012 Jun 18. PubMed PMID: 22587457. 2. Nakayama Y, Inoue Y, Minagawa N, Onitsuka K, Nagata J, Shibao K, Hirata K, Sako T, Nagata N, Yamaguchi K. Chemopreventive effect of 4-[3,5-Bis(trimethylsilyl) benzamido] benzoic acid (TAC-101) on MNU-induced colon carcinogenesis in a rat model. Anticancer Res. 2009 Jun;29(6):2059-65. PubMed PMID: 19528465. 3. Eshima K, Fukaya S, Sugimoto A, Mori T, Yokoi H, Yamamoto Y, Sugiura S, Honda S, Masuko N, Murakami K, Yamasaki Y, Kagechika H. Contribution of AP-1 interference induced by TAC-101 to tumor growth suppression in a hepatocellular carcinoma model. Tumour Biol. 2009;30(1):1-7. doi: 10.1159/000189712. Epub 2009 Jan 12. PubMed PMID: 19142034. 4. Higginbotham KB, Lozano R, Brown T, Patt YZ, Arima T, Abbruzzese JL, Thomas MB. A phase I/II trial of TAC-101, an oral synthetic retinoid, in patients with advanced hepatocellular carcinoma. J Cancer Res Clin Oncol. 2008 Dec;134(12):1325-35. doi: 10.1007/s00432-008-0406-2. Epub 2008 May 27. PubMed PMID: 18504614.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Orally Active Compound Library Clinical Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

Amsilarotene 125973-56-0 Cell Cycle/Checkpoint CDK AsPC-1 Apoptosis TAC-101 orally active Retinoid X receptors cancer Inhibitor RAR/RXR TAC 101 inhibit RMG-II MIAPaCa-2 BxPC-3 Am 555S Retinoic acid receptors TAC101 inhibitor

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