1. Metabolic Enzyme/Protease
    Autophagy
  2. RAR/RXR
    Autophagy
  3. AGN 194310

AGN 194310 (Synonyms: VTP-194310)

Cat. No.: HY-16681 Purity: 98.02%
Handling Instructions

AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively.

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

AGN 194310 Chemical Structure

AGN 194310 Chemical Structure

CAS No. : 229961-45-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 616 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 660 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1740 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2700 In-stock
Estimated Time of Arrival: December 31
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Description

AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2].

IC50 & Target[1]

RARα

3 nM (Kd)

RARβ

2 nM (Kd)

RARγ

5 nM (Kd)

In Vitro

AGN194310 potently inhibits colony formation by all three lines, with IC50 values of 16 nM for LNCaP cells; 18 nM for PC3 cells; and 34 nM for DU-145 cells[2].
AGN 194310 (50 nM, 100 nM; LNCaP, PC-3 and DU-145 cells) inhibits colony formation at concentrations of 50 nM and 100 nM alone and in combination with TTNPB[2].
AGN 194310 (1 μM; 72 hours; LNCaP cells) treatment results in 80% apoptosis[2].

Cell Viability Assay[2]

Cell Line: LNCaP, PC-3 and DU-145 cells.
Concentration: 50 nM, 100 nM
Incubation Time:
Result: When used together with 100 nM TTNPB, there was almost complete reversal of the growth inhibitory effect of 50 nM and partial reversal of the effect of 100 nM.

Apoptosis Analysis[2]

Cell Line: LNCaP cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Induced apoptosis in LNCaP cells.
In Vivo

AGN 194310 (0.5 mg/kg/day; oral gavage; every day; for 10 days; female C57Bl/6J mice) treatment increases the number of granulocytes across haemopoietic compartments. A significant increase in the frequency of granulocyte-progenitor cells is observed in the bone marrow of mice after treatment with AGN194310[3].

Animal Model: Female C57Bl/6J mice (Five-week-old (34-37 days))[3]
Dosage: 0.5 mg/kg/day
Administration: Oral gavage; every day; for 10 days
Result: The number of granulocytes was significantly increased across haemopoietic compartments. Progenitor cells containing granulocytes also increased significantly.
Molecular Weight

424.55

Formula

C₂₈H₂₄O₂S

CAS No.

229961-45-9

SMILES

CC(S1)(C)C=C(C2=CC=C(CC)C=C2)C3=C1C=CC(C#CC4=CC=C(C(O)=O)C=C4)=C3

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 : 50 mg/mL (117.77 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3554 mL 11.7772 mL 23.5544 mL
5 mM 0.4711 mL 2.3554 mL 4.7109 mL
10 mM 0.2355 mL 1.1777 mL 2.3554 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AGN 194310VTP-194310AGN194310AGN-194310VTP194310VTP 194310RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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AGN 194310
Cat. No.:
HY-16681
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