ONC212 [1807861-48-8]
Référence HY-111343-100mg
Conditionnement : 100mg
Marque : MedChemExpress
ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
ONC212 Chemical Structure
CAS No. : 1807861-48-8
This product is a controlled substance and not for sale in your territory.
Based on 4 publication(s) in Google Scholar
Description |
ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis[1]. |
|||||||||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target |
GPR132[1] |
|||||||||||||||||||||||||
Cellular Effect |
|
|||||||||||||||||||||||||
In Vitro |
Cell proliferation assay reveals that at least a ten-fold lower concentration of ONC212 is needed to achieve 50% growth inhibition in comparison to ONC201. ONC212 shows GI50 values in the range of 0.1 to 0.4 μM, while the corresponding ONC201 GI50 values are in the range of 4 to 9 μM for the seven pancreatic cancer cell lines tested. Long-term cell proliferation assay shows that both ONC201 and ONC212 are comparable in inhibiting colony formation at a 20 μM dose. However, at a 5 μM dose, ONC212 is about 50-times more potent than ONC201 in preventing colony formation in four out of the seven pancreatic cancer cell lines tested. Induction of apoptosis by ONC212 is an earlier event than ONC201. Treatment with ONC201 and ONC212 reduces the expression of anti-apoptotic markers such as XIAP and MCL-1. Western blot analysis shows that in the HPAF-II cell line, ATF4 and phosphorylated EIF2α are upregulated as early as 6 to 12 hours post ONC201 or ONC212 treatment[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
|||||||||||||||||||||||||
In Vivo |
Biweekly oral administration of 50 mg/kg ONC212 markedly inhibits Acute myeloid leukemia (AML) expansion and prolongs overall survival (p=0.0003). Median survival increases from 43 d in controls to 49 d in the ONC212-treated group (+14%)[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
|||||||||||||||||||||||||
Masse moléculaire |
440.46 |
|||||||||||||||||||||||||
Formule |
C24H23F3N4O |
|||||||||||||||||||||||||
CAS No. |
1807861-48-8 |
|||||||||||||||||||||||||
Appearance |
Solid |
|||||||||||||||||||||||||
Color |
White to off-white |
|||||||||||||||||||||||||
SMILES |
O=C1N(CC2=CC=C(C(F)(F)F)C=C2)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4 |
|||||||||||||||||||||||||
Livraison | Room temperature in continental US; may vary elsewhere. |
|||||||||||||||||||||||||
Stockage |
|
|||||||||||||||||||||||||
Solvant et solubilité |
In Vitro:
DMSO : 50 mg/mL (113.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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.
|
|||||||||||||||||||||||||
Pureté et documentation |
Purity: 99.32% |
|||||||||||||||||||||||||
Références |
|
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 2.2704 mL | 11.3518 mL | 22.7035 mL | 56.7588 mL |
5 mM | 0.4541 mL | 2.2704 mL | 4.5407 mL | 11.3518 mL | |
10 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL | 5.6759 mL | |
15 mM | 0.1514 mL | 0.7568 mL | 1.5136 mL | 3.7839 mL | |
20 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8379 mL | |
25 mM | 0.0908 mL | 0.4541 mL | 0.9081 mL | 2.2704 mL | |
30 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8920 mL | |
40 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL | |
50 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1352 mL | |
60 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9460 mL | |
80 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL | |
100 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5676 mL |
ONC212 Related Classifications
- Apoptosis
- Apoptosis