Amsilarotene

SKU: orb1306403

Description

Amsilarotene (TAC101) induces cell cycle arrest by inhibiting retinoblastoma (RB) protein phosphorylation and upregulating CDK inhibitors. It also exerts cytotoxic effects through downregulation of thymidylate synthase and cyclin A. This mechanism supports its research application in studying cancer cell proliferation in both in vitro and in vivo models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 125973-56-0
• MW: 385.6
• Purity: 99.27% (May vary between batches)
• Formula: C₂₀H₂₇NO₃Si₂
• SMILES: C[Si](C)(C)c1cc(cc(c1)[Si](C)(C)C)C(=O)Nc1ccc(cc1)C(O)=O
• Target: CDK,Apoptosis,Retinoid Receptor
• Solubility: DMSO:60 mg/mL (155.6 mM);H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.19 mM)

Bioactivity

• Target IC50:
  RARα:2.4 nM (Ki)|RARβ:400 nM (Ki)
• 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.
• 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Am 555S, BxPC-3, cancer, AsPC-1, Amsilarotene, Apoptosis, CDK, inhibit, MIAPaCa-2, Inhibitor, Retinoic acid receptors, Retinoid X receptors, RMG-II, TAC 101, TAC101, TAC-101, RAR/RXR, orally active

Compound Identifiers

PubChem CID

9800306