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Purity: ≥98%
KO-947 is a novel, potent and selective ERK1/2 kinase inhibitor that may be helpful in treating tumors with dysregulated MAPK pathways. Slow dissociation kinetics are exhibited by KO-947. The tumor cells that exhibit dysregulation of the MAPK pathway, including mutations in the BRAF, NRAS, or KRAS, proliferated and were effectively inhibited by KO-947. In preclinical models that are resistant to BRAF and MEK inhibitors, KO-947 also reduces MAPK signaling and cellular proliferation. KO-947 causes tumor regressions in tumor models with BRAF or RAS mutations as well as tumor models without BRAF or RAS mutations but with other MAPK pathway dysregulations.
| Targets |
ERK1; ERK2
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|---|---|
| ln Vitro |
KO-947 is an ERK inhibitor with at least 50-fold selectivity against a panel of 450 kinases that has a 10 nM concentration. In tumor cells with dysregulated MAPK pathway signaling, such as those with BRAF, NRAS, or KRAS mutations, KO-947 inhibits ERK signaling and proliferation at low nanomolar concentrations[1].
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| ln Vivo |
KO-947 induces regressions in RAS- and RAF-mutant melanoma, NSCLC, and pancreatic cancer models on administration schedules ranging from daily to weekly in cell-line derived xenograft studies and profoundly suppresses ERK signaling for up to five days after a single dose. Similar antitumor activity is made possible by intermittent dosing at a lower dose intensity[1].
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| References |
| Molecular Formula |
C21H17N5O
|
|---|---|
| Molecular Weight |
355.392583608627
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| Exact Mass |
355.14
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| Elemental Analysis |
C, 70.97; H, 4.82; N, 19.71; O, 4.50
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| CAS # |
1695533-89-1
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| Related CAS # |
1695533-89-1
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| Appearance |
Solid powder
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| SMILES |
C1C2=CC3=C(C=C2NC(=O)N1CC4=CC=CC=C4)NN=C3C5=CC=NC=C5
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| InChi Key |
ODIUJYZERXVGEI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17N5O/c27-21-23-18-11-19-17(20(25-24-19)15-6-8-22-9-7-15)10-16(18)13-26(21)12-14-4-2-1-3-5-14/h1-11H,12-13H2,(H,23,27)(H,24,25)
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| Chemical Name |
6-benzyl-3-pyridin-4-yl-5,8-dihydro-1H-pyrazolo[4,3-g]quinazolin-7-one
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| Synonyms |
KO-947; KO947; KO 947
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 62.5~71 mg/mL (175.9~199.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03051035 | Terminated | Drug: KO-947 | Advanced Malignant Neoplasm | Kura Oncology, Inc. | April 6, 2017 | Phase 1 |
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