2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Apoptosis
  3. RAR/RXR Apoptosis
  4. Amsilarotene

Amsilarotene  (Synonyms: TAC-101; Am 555S)

Cat. No.: HY-14653 Purity: 99.70%
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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.

For research use only. We do not sell to patients.

Amsilarotene Chemical Structure

Amsilarotene Chemical Structure

CAS No. : 125973-56-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 198 In-stock
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Solid
5 mg USD 180 In-stock
10 mg USD 290 In-stock
25 mg USD 580 In-stock
50 mg USD 930 In-stock
100 mg USD 1450 In-stock
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Based on 1 publication(s) in Google Scholar

Amsilarotene Related Antibodies

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Description

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 Vitro

Amsilarotene (0, 10, 25 μM; 24 hours) induces apoptosis of human epithelial ovarian carcinoma-derived cell lines in a concentration-dependent manner[2].
Amsilarotene (10, 20 μM; 0, 3, 6, and 9 days) inhibits the proliferation of BxPC-3 and MIAPaCa-2 cells[3].
Amsilarotene (10 μM; 48 hours) increases the proportion of sensitive BxPC-3 cells in the G1 phase[3].
Amsilarotene (10 μM; 0, 3, 6, 24, 48, 72 hours) inhibits the retinoblastoma-gene product (RB) phosphorylation in BxPC-3 cells between 24 and 72 hours[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Amsilarotene Related Antibodies

Apoptosis Analysis[2]

Cell Line: RMG-I, RMG-II, RTSG, RMUG-S, RMUG-L, and KF cells
Concentration: 0, 10, 25 μM
Incubation Time: 24 hours
Result: Induced apoptosis in a concentration-dependent manner in all of the cell lines, except KF cells.

Cell Proliferation Assay[3]

Cell Line: BxPC-3, MIAPaCa-2, AsPC-1 cells
Concentration: 10 and 20 μM
Incubation Time: 0, 3, 6, and 9 days.
Result: Inhibited the proliferation of BxPC-3 and MIAPaCa-2 cells, but not the proliferation of AsPC-1 cells.

Cell Cycle Analysis[3]

Cell Line: Sensitive BxPC-3 cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: The proportion of cells in the G1 phase increased from 43% of untreated control cells to 86%
In Vivo

Amsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Clinical Trial
Molecular Weight

385.60

Formula

C20H27NO3Si2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[Si](C)(C)C1=CC(C(NC2=CC=C(C(O)=O)C=C2)=O)=CC([Si](C)(C)C)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (259.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5934 mL 12.9668 mL 25.9336 mL
5 mM 0.5187 mL 2.5934 mL 5.1867 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.48 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5934 mL 12.9668 mL 25.9336 mL 64.8340 mL
5 mM 0.5187 mL 2.5934 mL 5.1867 mL 12.9668 mL
10 mM 0.2593 mL 1.2967 mL 2.5934 mL 6.4834 mL
15 mM 0.1729 mL 0.8645 mL 1.7289 mL 4.3223 mL
20 mM 0.1297 mL 0.6483 mL 1.2967 mL 3.2417 mL
25 mM 0.1037 mL 0.5187 mL 1.0373 mL 2.5934 mL
30 mM 0.0864 mL 0.4322 mL 0.8645 mL 2.1611 mL
40 mM 0.0648 mL 0.3242 mL 0.6483 mL 1.6209 mL
50 mM 0.0519 mL 0.2593 mL 0.5187 mL 1.2967 mL
60 mM 0.0432 mL 0.2161 mL 0.4322 mL 1.0806 mL
80 mM 0.0324 mL 0.1621 mL 0.3242 mL 0.8104 mL
100 mM 0.0259 mL 0.1297 mL 0.2593 mL 0.6483 mL
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Amsilarotene Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Amsilarotene125973-56-0TAC-101 Am 555STAC101TAC 101RAR/RXRApoptosisRetinoic acid receptorsRetinoid X receptorscancerorally activeBxPC-3MIAPaCa-2AsPC-1RMG-IIInhibitorinhibitorinhibit

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