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ONC212 

Cat. No.: HY-111343 Purity: 99.20%
Handling Instructions

ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer drug and also a selective agonist of GPR132.

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

ONC212 Chemical Structure

ONC212 Chemical Structure

CAS No. : 1807861-48-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 143 In-stock
Estimated Time of Arrival: December 31
5 mg USD 130 In-stock
Estimated Time of Arrival: December 31
10 mg USD 220 In-stock
Estimated Time of Arrival: December 31
25 mg USD 440 In-stock
Estimated Time of Arrival: December 31
50 mg USD 790 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
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Description

ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer drug and also a selective agonist of GPR132.

IC50 & Target

GPR132[1]

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].

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]. ONC212 treatment exhibits significantly greater growth inhibition in comparison to ONC201. A dose of 50 mg/kg of ONC212 administered three-times a week is sufficient to lead to significant growth inhibition of tumors compare to the control group for these two models. Results demonstrate that ONC212 treated tumors show reduced proliferation in the HPAF-II model[2]. In vivo toxicity assessment experiments show that ONC212 is well tolerated up to 250 mg/kg. 300 mg/kg of ONC212 causes splenic damage and elevates liver enzymes. ONC212 has a slightly shorter half-life than ONC201, with a clearance from the blood at 12 hours, T1/2 of 4.3 hours, and Cmax of 1.4 µg/mL[3].

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 (113.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2704 mL 11.3518 mL 22.7035 mL
5 mM 0.4541 mL 2.2704 mL 4.5407 mL
10 mM 0.2270 mL 1.1352 mL 2.2704 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 (5.68 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

All pancreatic cancer cell lines are treated with ONC201 or ONC212 at the indicated doses and time-points. Post-treatment, both floating and adherent cells are collected, fixed in 70% ethanol and stained with propidium iodide in the presence of ribonuclease A. Flow cytometric data is collected using a flow cytometer. The sub-G1 fraction (apoptotic) is quantified, and analysis is performed to quantify the distribution of cells in G1, S and G2-M phases of the cell cycle utilizing[2].

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

Animal Administration
[2]

Six- to seven-week-old female athymic nu/nu mice are used in this study. A total of 3 to 5×106 luciferase-expressing cells are suspended in 50 μL of PBS mixed with 50 μL of Matrigel and subcutaneously injected into the rear flanks of the mice. When tumor volume reaches an average of 100 to 150 cm3, mice are randomly assigned to the indicated control or treatment groups. ONC201 and ONC212 are delivered in a solution of 10% DMSO, 20% Kolliphor®EL and 70% PBS by oral gavage. The length (L) and width (W) of the tumors are measured 1 to 2 times a week using a digital caliper, and the volume of the tumor is calculated. Mice are also weighed once a week to monitor signs of drug toxicity[2].

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

References
Molecular Weight

440.46

Formula

C₂₄H₂₃F₃N₄O

CAS No.

1807861-48-8

SMILES

O=C1N(CC2=CC=C(C(F)(F)F)C=C2)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4

Shipping

Room temperature in continental US; may vary elsewhere

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ONC212
Cat. No.:
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ONC212

Cat. No.: HY-111343