KO-947

Name: KO-947
Brand: MedChemExpress
SKU: HY-112181
Rating: 5.0 (5 reviews)

Cat. No.: HY-112181 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.

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

KO-947 Chemical Structure

CAS No. : 1695533-89-1

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 259	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 897	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1639	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 5 publication(s) in Google Scholar

3 Publications Citing Use of MCE KO-947

: KO-947 purchased from MedChemExpress. Usage Cited in: Pediatr Res. 2023 May 3. [Abstract]; KO-947 (5 mM) inhibits the EGF-induced downregulated expression of CK19 and upregulated expression of N-cadherin in HIBEpic cells.

: KO-947 purchased from MedChemExpress. Usage Cited in: Pediatr Res. 2023 May 3. [Abstract]; KO-947 (5 mM) inhibits the EGF-induced increased expression of N-cadherin and decreased expression of E-cadherin in HIBEpic cells.

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Biological Activity
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Description

KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.

IC₅₀ & Target^[1]

ERK1

ERK2

In Vitro

KO-947 is a 10 nM inhibitor of ERK with at least 50-fold selectivity against a panel of 450 kinases. KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling, including mutations in BRAF, NRAS or KRAS, at low nanomolar concentrations^[1].

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

In Vivo

In cell-line derived xenograft studies, KO-947 profoundly suppresses ERK signaling for up to five days after a single dose and induces regressions in RAS- and RAF-mutant melanoma, NSCLC and pancreatic cancer models on administration schedules ranging from daily to weekly. Intermittent dosing enables comparable antitumor activity at reduced dose-intensity^[1].

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

Molecular Weight

355.39

Formula

C₂₁H₁₇N₅O

CAS No.

1695533-89-1

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=CC(NN=C3C4=CC=NC=C4)=C3C=C2CN1CC5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (175.86 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	2.8138 mL	14.0691 mL	28.1381 mL
5 mM	0.5628 mL	2.8138 mL	5.6276 mL
10 mM	0.2814 mL	1.4069 mL	2.8138 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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: ≥ 2.08 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.61%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (252 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Burrows F, et al. KO-947, a potent ERK inhibitor with robust preclinical single agent activity in MAPK pathway dysregulated tumors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, D

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8138 mL	14.0691 mL	28.1381 mL	70.3453 mL
	5 mM	0.5628 mL	2.8138 mL	5.6276 mL	14.0691 mL
	10 mM	0.2814 mL	1.4069 mL	2.8138 mL	7.0345 mL
	15 mM	0.1876 mL	0.9379 mL	1.8759 mL	4.6897 mL
	20 mM	0.1407 mL	0.7035 mL	1.4069 mL	3.5173 mL
	25 mM	0.1126 mL	0.5628 mL	1.1255 mL	2.8138 mL
	30 mM	0.0938 mL	0.4690 mL	0.9379 mL	2.3448 mL
	40 mM	0.0703 mL	0.3517 mL	0.7035 mL	1.7586 mL
	50 mM	0.0563 mL	0.2814 mL	0.5628 mL	1.4069 mL
	60 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1724 mL
	80 mM	0.0352 mL	0.1759 mL	0.3517 mL	0.8793 mL
	100 mM	0.0281 mL	0.1407 mL	0.2814 mL	0.7035 mL

KO-947 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:

KO-9471695533-89-1KO947KO 947ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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KO-947

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KO-947 Related Antibodies

3 Publications Citing Use of MCE KO-947

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•Related Screening Libraries:

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View All ERK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

KO-947 Related Antibodies

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Complete Stock Solution Preparation Table

KO-947 Related Classifications

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