1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. KO-947

KO-947 

Cat. No.: HY-112181
Handling Instructions

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

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

KO-947 Chemical Structure

KO-947 Chemical Structure

CAS No. : 1695533-89-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 260 In-stock
Estimated Time of Arrival: December 31
25 mg USD 490 Get quote
50 mg USD 690 Get quote
100 mg USD 950 Get quote
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Description

KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential clinical 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].

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (175.86 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 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

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
Molecular Weight

355.39

Formula

C₂₁H₁₇N₅O

CAS No.

1695533-89-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

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The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
KO-947
Cat. No.:
HY-112181
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KO-947

Cat. No.: HY-112181