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ONC212 GPR agonist

Name: ONC212
Brand: Selleck Chemicals
SKU: S8673
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S8673

ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. This compound is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.

Chemical Structure

Molecular Weight: 440.46

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S867301 DMSO]88 mg/mL]false]Ethanol]88 mg/mL]false]Water]Insoluble]false Purity: 99.87%

99.87

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Chemical Information, Storage & Stability

Molecular Weight	440.46	Formula	C₂₄H₂₃F₃N₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1807861-48-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN(CC2=C1N3CCN=C3N(C2=O)CC4=CC=C(C=C4)C(F)(F)F)CC5=CC=CC=C5

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 88 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.200mg/ml (4.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 44 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.400mg/ml (3.18mM)	Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	ONC212 shows an anti-proliferative effect in a large panel of pancreatic cancer cell lines with this compound having at least a ten-fold increased potency than ONC201. It induces apoptosis earlier and at lower concentrations than ONC201 in sensitive pancreatic cancer cell lines^[1]. This compound exerts potent and prominent apoptogenic effects on acute myeloid leukemia (AML) and mantle cell lymphoma (MCL) cell lines (e.g., ED50s of 141.0 nM in p53 wild-type OCI-AML3 cells, 105.7 nM in MOLM13 cells, and 265.2 nM in p53-null JeKo-1 cell lines). Time course analysis of apoptosis in OCI-AML3 cells shows that it takes more than 36 hours to start to induce apoptosis^[2]. This chemical significantly induces Sub-G1 apoptotic cells and/or cell cycle arrest^[4].
In vivo	ONC212 shows improved efficacy in melanoma and hepatocellular carcinoma xenograft models^[1]. This compound has a broad therapeutic window, an acceptable PK profile, and is orally well-tolerated in mice with no evidence of toxicity at efficacious doses in both colon and triple negative breast cancer^[3]. It exhibits rapid kinetics of activity. This chemical has a slightly shorter half-life than ONC201, with a clearance from the blood at 12 hours, T_1/2 of 4.3 hours, and Cmax of 1.4 mg/mL. It has a prolonged pharmacodynamic effect despite systemic clearance. Oral administration shows potent anti-tumor efficacy in a human melanoma xenograft and hepatocellular model. ONC206 and ONC201 both inhibit invasion and migration of tumor cells while this compound inhibits only invasion^[4].
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5669847/ [2] http://www.bloodjournal.org/content/128/22/4059 [3] http://cancerres.aacrjournals.org/content/77/13_Supplement/3245 [4] https://pubmed.ncbi.nlm.nih.gov/28489985/

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