Cat. No.: HY-112424

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Tinodasertib

(Synonyms: ETC-206)

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Tinodasertib (ETC-206) is a selective MNK1 and MNK2 inhibitor with IC₅₀s of 64 nM and 86 nM, respectively.

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Pureté: 99.60%
CAS No.: 1464151-33-4
Formule: C₂₅H₂₀N₄O₂
Masse moléculaire:408.45

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tinodasertib Chemical Structure

CAS No.: 1464151-33-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Tinodasertib (ETC-206) is a selective MNK1 and MNK2 inhibitor with IC₅₀s of 64 nM and 86 nM, respectively.

IC₅₀ & Target^[1]

MNK1

64 nM (IC₅₀)

MNK2

86 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform MNK :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	26.3 μM Compound: ETC-206; 2	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
DOHH-2	IC₅₀	1.624 μM Compound: 1; ETC-206	Antiproliferative activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33971490]
DOHH-2	IC₅₀	15.3 μM Compound: ETC-206; 2	Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
HEK293	IC₅₀	64 nM Compound: ETC-206	Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis	[PMID: 30530193]
HEK293	IC₅₀	86 nM Compound: ETC-206	Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis	[PMID: 30530193]
HT-29	IC₅₀	>50 μM Compound: ETC-206; 2	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
MDA-MB-231	IC₅₀	35.5 μM Compound: ETC-206; 2	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
PANC-1	IC₅₀	>50 μM Compound: ETC-206; 2	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
PC-3	IC₅₀	>50 μM Compound: ETC-206; 2	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
TMD8	IC₅₀	2.138 μM Compound: 1; ETC-206	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33971490]
TMD8	IC₅₀	27 μM Compound: ETC-206; 2	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]

In Vitro

Tinodasertib (ETC-206) inhibits eIF4E phosphorylation in HeLa cell line with an IC₅₀ of 321 nM. The anti-proliferative effects of ETC-206 are assessed in vitro, using CellTiter-Glo viability assay against 25 hematological cancer cell lines including the K562 cell line that overexpresses eIF4E (K562 o/e eIF4E). The IC₅₀s are 1.71 μM, 3.36 μM, 3.70 μM, 4.81 μM, 5.13 μM, 5.05 μM, 6.70 μM, 9.76 μM, and 48.8 μM for SU-DHL-6, GK-5, MC 116, P3HR-1, DOHH2, MPC-11, Ramos.2G6.4C10, AHH-1, and K562 o/e eIF4E cells, respectively^[1].

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

In Vivo

The antitumor effect of ETC-206 is then assessed in a K562 e/o eIF4E mouse xenograft model after oral administration at 25, 50, or 100 mg/kg alone or in combination with a 2.5 mg/kg fixed dose of Dasatinib throughout the study. Dasatinib at 2.5 mg/kg elicits a tumor growth inhibition (TGI) of 88% with one tumor-free animal. In contrast, ETC-206 alone only yields a maximum TGI of 23% at the highest administered dose of 100 mg/kg, which does not impede tumor growth, and is similar to the nontreated animals. ETC-206 with 2.5 mg/kg of Dasatinib not only increases tumor growth inhibition in a dose-dependent manner but, more importantly leads to 2, 5, and 8 out of 8 tumor-free animals at 25, 50, and 100 mg/kg, respectively. The combination of ETC-206 and Dasatinib inhibits tumor growth at all tested doses, and no weight loss is recorded. Both the combination of ETC-206 and Dasatinib and, on the other hand, the dual MNK1/2 and BCR-ABL1 inhibitors prevent tumor growth in the same mouse xenograft model. ETC-206 has moderate terminal elimination half-life (t_1/2=1.7 h, and 1.77 h for mouse (1 mg/kg, i.v.), mouse (5 mg/kg, p.o.))^[1].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1464151-33-4
Appearance Solid
Masse moléculaire 408.45
Formule C₂₅H₂₀N₄O₂
Color Light yellow to yellow
SMILES

N#CC1=CC=C(C2=CN=C3C=CC(C4=CC=C(C(N5CCOCC5)=O)C=C4)=CN32)C=C1
Synonyms

ETC-206
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Redox Biol

Targeting ALDH1A1 to enhance the efficacy of KRAS-targeted therapy through ferroptosis. [Abstract]

2024 Nov:77:103361. PMID: 39317105

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (122.41 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4483 mL

12.2414 mL

24.4828 mL

5 mM

0.4897 mL

2.4483 mL

4.8966 mL

10 mM

0.2448 mL

1.2241 mL

2.4483 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (12.24 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

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

Solubility: ≥ 5 mg/mL (12.24 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.24 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

The anti-proliferative effects of ETC-206 are assessed in vitro, using CellTiter-Glo viability assay against 25 hematological cancer cell lines including the K562 cell line that overexpresses eIF4E (K562 o/e eIF4E). The IC₅₀s are in general in the micromolar range^[1].

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

Animal Administration^[1]

Mice^[1]
CD-1 female mice (6-8 weeks old) are weighed, and those selected for dosing are 24±2 g. Three mice are randomly grouped per time point. Mice are administered a single dose of 1 mg/kg of ETC-206 via tail vein injection or a single dose of 5 mg/kg of ETC-206 via oral gavage. The volume of injection for intravenous (i.v.) and oral (p.o.) administration is 4 mL/kg and 8 mL/kg, respectively^[1].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Yang H, et al. Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia. J Med Chem. 2018 May 24;61(10):4348-4369. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.4483 mL	12.2414 mL	24.4828 mL	61.2070 mL
	5 mM	0.4897 mL	2.4483 mL	4.8966 mL	12.2414 mL
	10 mM	0.2448 mL	1.2241 mL	2.4483 mL	6.1207 mL
	15 mM	0.1632 mL	0.8161 mL	1.6322 mL	4.0805 mL
	20 mM	0.1224 mL	0.6121 mL	1.2241 mL	3.0604 mL
	25 mM	0.0979 mL	0.4897 mL	0.9793 mL	2.4483 mL
	30 mM	0.0816 mL	0.4080 mL	0.8161 mL	2.0402 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	1.2241 mL
	60 mM	0.0408 mL	0.2040 mL	0.4080 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

Keywords

Tinodasertib

1 Cited Publications

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Tinodasertib

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Publications Citing Use of MedChemExpress (MCE) Tinodasertib

Voir tous les produits spécifiques à Isoform MNK

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tinodasertib

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Oxygen Sensing Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Tinodasertib

Voir tous les produits spécifiques à Isoform MNK

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tinodasertib Related Classifications

HY-112424 Related Classifications