2. Apoptosis Metabolic Enzyme/Protease Epigenetics Cell Cycle/DNA Damage
  3. Apoptosis Mitochondrial Metabolism Caspase PARP
  4. ONC213

ONC213 is an orally active αKGDH inhibitor. ONC213 can suppress mitochondrial respiration and elevate α-ketoglutarate levels by inhibiting αKGDH activity. ONC213 can induce cells apoptosis by inducing mitochondrial stress response and inhibiting translation of MCL-1. ONC213 can be used for the research of cancer, such as acute myeloid leukemia research (AML).

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ONC213

ONC213 Chemische Struktur

CAS. Nr. : 1977540-13-8

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ONC213 Related Antibodies

Top Publications Citing Use of Products

Alle Caspase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Alle PARP Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Beschreibung

ONC213 is an orally active αKGDH inhibitor. ONC213 can suppress mitochondrial respiration and elevate α-ketoglutarate levels by inhibiting αKGDH activity. ONC213 can induce cells apoptosis by inducing mitochondrial stress response and inhibiting translation of MCL-1. ONC213 can be used for the research of cancer, such as acute myeloid leukemia research (AML)[1].

IC50 & Target[1]

Caspase 3

 

In Vitro

ONC213 (500 nM, 48 h) reduces colony formation in primary AML samples[1].
ONC213 (125-1000 nM, 48 h) induces apoptosisi in MV4-11, OCI-AML3, and MOLM-13 cells[1].
ONC213 (250-500 nM, 8 h) strongly suppresses maximal OCR and spare respiratory capacity, with a minimal effect on basal respiration in MV4-11 and THP-1 cells[1].
ONC213 (500 nM, 0.5-16 h) inhibits activity of α-KGDH in MV4-11 cells[1].
ONC213 (250-500 nM, 4-8 h) induces mitochondrial stress gene expression in MV4-11 cells[1].

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

ONC213 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV4-11, OCI-AML3, and MOLM-13 cells
Concentration: 125, 250, 500 and 1000 nM
Incubation Time: 48 h
Result: Increased apoptotic/dead cells.
Increased cleavage of caspase 3 and PARP.
In Vivo

ONC213 (75-125 mg/kg, p.o., daily for 8 days) prolongs survival in MV4-11 xenograft mice[1].

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

Animal Model: MV4-11 xenografted mice models[1]
Dosage: 75 and 125 mg/kg
Administration: Orally administration, daily for 8 days
Result: Increased median survival to 43.5 days from 33 days at75 mg/kg.
Nearly doubled survival from 33 to 62 days at125 mg/kg.
Molekulargewicht

408.44

Formel

C23H22F2N4O
CAS. Nr.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (244.83 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 2.4483 mL 12.2417 mL 24.4834 mL
5 mM 0.4897 mL 2.4483 mL 4.8967 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4483 mL 12.2417 mL 24.4834 mL 61.2085 mL
5 mM 0.4897 mL 2.4483 mL 4.8967 mL 12.2417 mL
10 mM 0.2448 mL 1.2242 mL 2.4483 mL 6.1209 mL
15 mM 0.1632 mL 0.8161 mL 1.6322 mL 4.0806 mL
20 mM 0.1224 mL 0.6121 mL 1.2242 mL 3.0604 mL
25 mM 0.0979 mL 0.4897 mL 0.9793 mL 2.4483 mL
30 mM 0.0816 mL 0.4081 mL 0.8161 mL 2.0403 mL
40 mM 0.0612 mL 0.3060 mL 0.6121 mL 1.5302 mL
50 mM 0.0490 mL 0.2448 mL 0.4897 mL 1.2242 mL
60 mM 0.0408 mL 0.2040 mL 0.4081 mL 1.0201 mL
80 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7651 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6121 mL
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ONC213 Related Classifications

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:

ONC2131977540-13-8ONC 213ONC-213ApoptosisMitochondrial MetabolismCaspasePARPpoly ADP ribose polymeraseαKGDHα-ketoglutarateMitochondrial stressMCL-1AMLMV4-11Inhibitorinhibitorinhibit

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