Amsilarotene

SKU: orb1306403

Description

Amsilarotene

Research Area

Cell Biology, Metabolism Research

Images & Validation

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Key Properties

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CAS Number	125973-56-0
MW	385.6
Purity	99.27%
Formula	C₂₀H₂₇NO₃Si₂
SMILES	C[Si](C)(C)c1cc(cc(c1)[Si](C)(C)C)C(=O)Nc1ccc(cc1)C(O)=O
Target	Retinoid Receptor,CDK,Apoptosis
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

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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 examin 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 considere the maximum tolerated dose and 20 mg/da 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. Read more...
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). Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Disclaimer	For research use only

Alternative Names

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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

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Compound Identifiers

PubChem CID

9800306 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	125973-56-0
MW:	385.6
Formula:	C₂₀H₂₇NO₃Si₂

Amsilarotene

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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