Temuterkib (Synonyms: LY3214996)

Name: Temuterkib
Brand: MedChemExpress
SKU: HY-101494
Rating: 5.0 (29 reviews)

Cat. No.: HY-101494 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC₅₀ of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.

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

Temuterkib Chemical Structure

CAS No. : 1951483-29-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 225	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 675	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1000	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 29 publication(s) in Google Scholar

28 Publications Citing Use of MCE Temuterkib

: Temuterkib purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2019 May;110(5):1746-1759. [Abstract]; Cells are treated with RA in the presence or absence of the Erk1/2 inhibitor LY3214996, phospho-Erk1/2, Erk1/2, phospho-JNK, JNK, phospho-c-Jun, c-Jun, total and cleaved PARP, phospho-STAT3S727, and STAT3 are analyzed.

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ERK ERK1 ERK2 ERK5 ERK8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ERK1

5 nM (IC₅₀)

ERK2

5 nM (IC₅₀)

In Vitro

Temuterkib is a highly selective inhibitor of ERK1 and ERK2, with IC₅₀ of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to Temuterkib^[1].

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

In Vivo

In tumor xenograft models, Temuterkib inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. Temuterkib shows either similar or superior anti-tumor activity as compared to other published ERK inhibitors in BRAF or RAS mutant cell lines and xenograft models. Oral administration of single-agent Temuterkib significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models. Therefore, Temuterkib can be tailored for treatment of cancers with MAPK pathway alteration. In addition, Temuterkib has anti-tumor activity in a PLX4032-resistant A375 melanoma xenograft model due to MAPK reactivation, may have potential for treatment of melanoma patients who have failed BRAF therapies. More importantly, Temuterkib can be combined with investigational and approved agents in preclinical models, particularly KRAS mutant models. Combination treatment of Temuterkib and CDK4/6 inhibitor abemaciclib is well tolerated and results in potent tumor growth inhibition or regression in multiple in vivo cancer models, including KRAS mutant colorectal and non-small cell lung cancers^[1].

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

Clinical Trial

Molecular Weight

453.56

Formula

C₂₂H₂₇N₇O₂S

CAS No.

1951483-29-6

Appearance

Solid

Color

White to yellow

SMILES

O=C(C(C=C(C1=NC(NC2=CC=NN2C)=NC=C1)S3)=C3C4(C)C)N4CCN5CCOCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 20 mg/mL (44.10 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	2.2048 mL	11.0239 mL	22.0478 mL
5 mM	0.4410 mL	2.2048 mL	4.4096 mL
10 mM	0.2205 mL	1.1024 mL	2.2048 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (254 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Shripad V. Bhagwat, et al. Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Cancer Research. July 2017.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2048 mL	11.0239 mL	22.0478 mL	55.1195 mL
	5 mM	0.4410 mL	2.2048 mL	4.4096 mL	11.0239 mL
	10 mM	0.2205 mL	1.1024 mL	2.2048 mL	5.5119 mL
	15 mM	0.1470 mL	0.7349 mL	1.4699 mL	3.6746 mL
	20 mM	0.1102 mL	0.5512 mL	1.1024 mL	2.7560 mL
	25 mM	0.0882 mL	0.4410 mL	0.8819 mL	2.2048 mL
	30 mM	0.0735 mL	0.3675 mL	0.7349 mL	1.8373 mL
	40 mM	0.0551 mL	0.2756 mL	0.5512 mL	1.3780 mL

Temuterkib 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:

Temuterkib1951483-29-6LY3214996LY 3214996LY-3214996ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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Temuterkib (Synonyms: LY3214996)

Customer Review

Temuterkib Related Antibodies

28 Publications Citing Use of MCE Temuterkib

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View All ERK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Temuterkib Related Antibodies

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Complete Stock Solution Preparation Table

Temuterkib Related Classifications

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