066ATZ
066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A Ki 100 nM and PIP4K2B Ki 800 nM. 066ATZ binds to ATP-binding sites of PIP4K2A and PIP4K2B to block lipid kinase activity. 066ATZ can be used for the research of non-small cell lung cancer.
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- Fòrmula: C22H23N11OS
- Peso molecular:489.56
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Help & FAQs
Actividad biológica
066ATZ (0.03-20 μM;) potently and selectively inhibits recombinant PIP4K2A (Ki = 170 nM) and PIP4K2B (Ki = 870 nM) in vitro[1].
066ATZ (0.5 μM) demonstrates high selectivity against most human protein kinases, with only CK2a and CK2a2 showing significant inhibition[1].
066ATZ (20 μM; 3 days) does not affect the in vitro growth rate of H1975* NSCLC cells[1].
066ATZ (20 μM) reduces the growth-promoting activity of M2a-polarized THP-1 macrophages towards H1975 NSCLC cells in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 NSCLC cells
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Concentration:20 μM
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Incubation Time:3 days
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Result:Had no effect on the growth rate of cultured H1975 cells, with cell number fold-change matching that of DMSO-treated control cells.
066ATZ (10-100 mg/kg; i.p.; single dose; 4 consecutive daily doses) is well tolerated at doses up to 100 mg/kg in female nude mice, and causes a transient blood glucose drop at doses of 30 mg/kg and higher[1].
066ATZ (10 mg/kg; i.p.; single dose) has a short in vivo half-life of ~0.5 h in male C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rag2/IL2RG double knockout (R2G2) (female, 7 weeks old, 1 × 107 H1975 cells was injected subcutaneously to establish a xenograft model)[1]
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Dosage:100 mg/kg
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Administration:i.p.; 5 times per week for 36 days
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Result:Reduced average tumor volume significantly compared to vehicle control on day 24 of treatment (p < 0.01).
Showed a small increase in CD31 staining in tumor tissues, indicating enhanced angiogenesis.
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Animal Model:nude (female)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:i.p.; single dose; 4 consecutive daily doses (100 mg/kg only)
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Result:Caused a transient 14% blood sugar drop 30 min after injection in the 30 mg/kg and 100 mg/kg groups, but not in the 10 mg/kg group.
Showed no difference in steady-state blood glucose after 4 consecutive daily doses of 100 mg/kg.
Did not affect body weight at a dose of 100 mg/kg.
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Animal Model:C57BL/6 (male)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Reached a maximum plasma concentration (Cmax) of 2,484 ng/mL (~5.1 μM) after a single dose.
Had a half-life (t1/2) of ~0.5 h.
Chemical Information
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Peso molecular 489.56
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Fòrmula C22H23N11OS
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SMILES
CN1C([C@H](N(C2=NC(NC3=CN=C(S3)C4=NNN=N4)=NC=C21)C5CCCC5)CC6=NC=CC=C6)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
066ATZ Related Classifications
HY-183627 Related Classifications
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