MU1210
Based on 1 Customer Validation
MU1210 (compound 12f), a chemical probe, is an inhibitor of CDC-like kinases Clk1, Clk2, and Clk4 (with IC50 values of 8, 20, and 12 nM respectively), with IC50 for HIPK1 and DYRK2 are 187 and 1309 nM. MU1210 also has favorable pharmacokinetic characteristics (in mice, 10 mg/kg, intraperitoneal injection: Cmax=1.24 μM, T1/2=58 minutes; no acute toxicity observed).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.5%
- CAS. Nr.: 2275601-87-9
- Formel: C22H16N4O
- Molecular Weight:352.39
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
Beschreibung
IC50 & Target
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CLK1 8 nM (IC50) |
CLK2 20 nM (IC50) |
CLK4 12 nM (IC50) |
HIPK1 187 nM (IC50) |
DYRK2 1309 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-22 | IC50 |
2.6 μM
Compound: 49; MU1210
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
| MCF7 | IC50 |
4.6 μM
Compound: MU1210
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by CyQuant assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by CyQuant assay
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[PMID: 33636538] |
Chemical Information
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CAS. Nr. 2275601-87-9
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Appearance Solid
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Molecular Weight 352.39
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Formel C22H16N4O
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Color White to off-white
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SMILES
CN1N=CC(C2=NC3=C(C=C2)OC=C3C4=CC=CC(C5=CC=NC=C5)=C4)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protokoll
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
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Acute Systemic Toxicity Study
Acute systemic toxicity studies evaluate adverse effects occurring after a single exposure, or repeated exposure within a short acute window, and the main in vivo readouts are mortality, moribund condition, clinical signs, body-weight change, and gross pathological findings; acute oral toxicity methods were developed to replace classical LD50 testing with reduced-animal designs such as fixed-dose procedure, acute toxic class method, and up-and-down procedure. The fixed-dose procedure classifies acute toxicity by administering predefined dose levels and observing evident toxicity rather than using death as the primary endpoint, whereas the acute toxic class method uses sequential groups of three animals per step and the up-and-down procedure doses animals sequentially to estimate an LD50 with fewer animals than conventional LD50 testing.
Reinheit & Dokumentation
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)