ONC212

Name: ONC212
Brand: MedChemExpress
SKU: HY-111343
Rating: 5.0 (5 reviews)

製品番号: HY-111343 純度: 99.86%: Data Sheet SDS COA 取扱説明書
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ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.

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ONC212 構造式

CAS 番号 : 1807861-48-8

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 143	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 143	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$130	在庫あり	Estimated Time of Arrival: December 31
10 mg	$220	在庫あり	Estimated Time of Arrival: December 31
25 mg	$360	在庫あり	Estimated Time of Arrival: December 31
50 mg	$560	在庫あり	Estimated Time of Arrival: December 31
100 mg	$840	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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Based on 5 publication(s) in Google Scholar

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製品説明

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

Cell Line	Type	Value	Description	References
Z-138	IC₅₀	49 1 Compound: 35; ONC212	Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay	[PMID: 33656892]
OCI-AML2	IC₅₀	76 1 Compound: 35; ONC212	Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry	[PMID: 33656892]
HCT-116	IC₅₀	0.11 3 Compound: ONC212	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 39172943]
OCI-AML-3	IC₅₀	60 1 Compound: 35; ONC212	Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry	[PMID: 33656892]
OCI-AML-3	IC₅₀	60 1 Compound: 35; ONC212	Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry	[PMID: 33656892]
OCI-AML2	IC₅₀	76 1 Compound: 35; ONC212	Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry	[PMID: 33656892]
SUM-159-PT	IC₅₀	77 1 Compound: 35; ONC212	Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 33656892]
HL-60	IC₅₀	0.09 3 Compound: ONC212	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 39172943]
Z-138	IC₅₀	49 1 Compound: 35; ONC212	Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay	[PMID: 33656892]
SUM-159-PT	IC₅₀	77 1 Compound: 35; ONC212	Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 33656892]
MIA PaCa-2	IC₅₀	0.1 3 Compound: ONC212	Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 39172943]
OCI-AML-3	IC₅₀	60 1 Compound: 35; ONC212	Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry Cytotoxicity against human OCI-AML-3 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry	[PMID: 33656892]
OCI-AML2	IC₅₀	76 1 Compound: 35; ONC212	Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry Cytotoxicity against human OCI-AML2 cells assessed as cell growth inhibition measured after 72 hrs by spectrophotometry	[PMID: 33656892]
SUM-159-PT	IC₅₀	77 1 Compound: 35; ONC212	Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition measured after 72 hrs by MTS assay	[PMID: 33656892]
Z-138	IC₅₀	49 1 Compound: 35; ONC212	Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay Antiproliferative activity against human Z138 cells transfected with D190A mutant in NSG mouse assessed as tumor reduction at 50 mg/kg/d, po administered via oral gavage for every 2 day measured after 31 days by luminescence assay	[PMID: 33656892]

体外実験

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.

体内実験

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, T_1/2 of 4.3 hours, and C_max of 1.4 μg/mL^[3].

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

分子量

440.46

分子式

C₂₄H₂₃F₃N₄O

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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 20% Cremophor EL 70% ddH2O
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution
Protocol 2

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

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 3

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

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 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.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

純度とドキュメンテーション

純度: 99.86%

Select Batch:

データシート (279 KB) SDS (701 KB)

COA (246 KB) HNMR (254 KB) LCMS (90 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Takenobu Nii, et al. The Novel Imipridone ONC212 Induces Pronounced Anti-Leukemia Effects in Vitro and In Vivo and Is Highly Synergistic with the BCL-2 Inhibitor ABT-199. ASH. 2017.

[2]. Lev A, et al. Anti-pancreatic cancer activity of ONC212 involves the unfolded protein response (UPR) and is reduced by IGF1-R and GRP78/BIP. Oncotarget. 2017 Sep 12;8(47):81776-81793. [Content Brief]

[3]. Wagner J, et al. Preclinical evaluation of the imipridone family, analogs of clinical stage anti-cancer small molecule ONC201, reveals potent anti-cancer effects of ONC212. Cell Cycle. 2017 Oct 2;16(19):1790-1799. [Content Brief]

細胞実験 ^[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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Takenobu Nii, et al. The Novel Imipridone ONC212 Induces Pronounced Anti-Leukemia Effects in Vitro and In Vivo and Is Highly Synergistic with the BCL-2 Inhibitor ABT-199. ASH. 2017. [2]. Lev A, et al. Anti-pancreatic cancer activity of ONC212 involves the unfolded protein response (UPR) and is reduced by IGF1-R and GRP78/BIP. Oncotarget. 2017 Sep 12;8(47):81776-81793. [Content Brief] [3]. Wagner J, et al. Preclinical evaluation of the imipridone family, analogs of clinical stage anti-cancer small molecule ONC201, reveals potent anti-cancer effects of ONC212. Cell Cycle. 2017 Oct 2;16(19):1790-1799. [Content Brief]

Complete Stock Solution Preparation Table

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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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:

ONC2121807861-48-8ONC 212ONC-212ApoptosisInhibitorinhibitorinhibit

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ONC212

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ONC212 関連抗体

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おすすめ

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•関連小分子:

•関連タンパク質:

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純度とドキュメンテーション

参考文献

カスタマーレビュー

ONC212 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ONC212 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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