| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C15H14N4O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
MRT00033659 is a potent, broad-spectrum kinase inhibitor acting on CK1 (IC50 0.9 μM for CK1δ) and CHK1 (IC50 0.23 μM). As a pyrazolo-pyridine analogue, it induces activation of the p53 pathway and destabilization of E2F-1[1]. It is supplied as an off-white to light yellow solid (C15H14N4O, MW 266.30) at 98.40% purity.
Physical & Chemical Properties
| CAS Number | 1401731-54-1 |
|---|---|
| Molecular Formula | C15H14N4O |
| Molecular Weight | 266.30 g/mol |
| Purity | 98.40% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | CC1=NNC2=NC=C(C=C21)C3=CC=CC(NC(C)=O)=C3 |
| Target | CK1δ, Chk1 |
| Signaling Pathway | Cell Cycle/DNA Damage; Stem Cell/Wnt; Apoptosis |
| Solubility | In Vitro: DMSO: 83.33 mg/mL (312.92 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. The compound is unstable in solutions, freshly prepared is recommended. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
CK1δ 0.9 μM (IC50) |
Chk1 0.23 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 83.33 mg/mL (312.92 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
The manufacturer notes that the compound is unstable in solution; prepare solutions fresh before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 4.17 mg/mL (15.66 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 4.17 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (41.7 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 4.17 mg/mL (15.66 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 4.17 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (41.7 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 4.17 mg/mL (15.66 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 4.17 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (41.7 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
At 5 μM, MRT00033659 (5-40 μM; 48 hours) is sufficient to significantly reduce cell number[1]. MRT00033659 (1-80 μM; 48 hours) causes substantial cell death starting at 5 μM[1]. Across 0.2-80 μM (48 hours), MRT00033659 produces robust and sustained stabilization of p53, MDM2 and p21 proteins, together with E2F-1 destabilization from 0.2 μM to 5 μM[1]. p38α MAPK is not inhibited by MRT00033659[1].
Cell Viability Assay[1]
| Cell Line | A375 cells |
|---|---|
| Concentration | 5, 20, 40 μM |
| Incubation Time | 48 hours |
| Result | Significantly reduced cell number of 5 μM. |
Apoptosis Analysis[1]
| Cell Line | A375 cells |
|---|---|
| Concentration | 1, 5, 10, 20, 40, 80 μM |
| Incubation Time | 48 hours |
| Result | Induced substantial cell death from 5 μM. |
Western Blot Analysis[1]
| Cell Line | A375 cells |
|---|---|
| Concentration | 0.2, 1, 5, 10, 20, 40, 80 μM |
| Incubation Time | 48 hours |
| Result | Induced a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 μM to 5 μM. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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