NN-01-195
NN-01-195 is a HSP90 and AURKA inhibitor. NN-01-195 binds tightly to and inhibits AURKA and HSP90, with an IC50 of 3.1 nM against AURKA and an IC50 of 8.7 nM against HSP90α. NN-01-195 induces mitotic arrest and spindle abnormality in tumor cells, and triggers cell apoptosis. NN-01-195 can be used in the research of solid tumors.
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- Formule: C56H60Cl2F4N12O5
- Masse moléculaire:1128.05
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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HSP90α 8.7 nM (IC50) |
NN-01-195 (1-10000 nM) can efficiently enter HEK293T cells and bind to intracellular HSP90, without showing obvious cell permeability limitations[1].
NN-01-195 (0-10 μM; 24-72 hours) reduces the viability of FaDu and NCI-H1975 cells, and induces G2/M cell cycle arrest, apoptosis and mitotic spindle abnormalities[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FaDu, NCI-H1975
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Concentration:500 and 1000 nM
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Incubation Time:72 h (cleaved PARP); 24 h (other targets)
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Result:Induced cleaved PARP (a marker of apoptosis) in FaDu and NCI-H1975 cells.
Induced total AURKA expression and reduced p-AURKA levels in FaDu cells, did not alter HSP70 or HSP60 expression, and did not reduce p-S6, total S6, p-AKT, total AKT, p-ERK, or total ERK levels.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUClast | AUCinf |
|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 0.500 h | 9870 ng/mL | 1.76 h | 24114 ng·h/mL | 26494 ng·h/mL |
NN-01-195 (30 mg/kg; i.p.; daily; 14 days) and Adavosertib (HY-10993) inhibits the growth of FaDu xenograft tumors in mice[1].
NN-01-195 (30 mg/kg; i.p.; daily; 21 days) exerts inhibitory effects on the growth of H1975 xenograft tumors in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG treated FaDu (6-10 weeks old, initial body weight 20-31 g)[1]
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Dosage:30 mg/kg (single-agent); 30 mg/kg (combination with 60 mg/kg adavosertib)
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Administration:i.p.; daily; 14 days
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Result:Did not cause a statistically significant reduction in tumor volume versus vehicle as a single agent.
Resulted in a statistically significant reduction in tumor volume versus vehicle, single-agent NN-01-195, single-agent adavosertib, and the VIC-1911 plus adavosertib combination when used in combination with adavosertib.
Led to a significantly lower Ki-67 H-score in tumor tissue in the NN-01-195 plus adavosertib group versus vehicle.
Caused no significant changes in body weight in any treatment group.
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Animal Model:NSG treate H1975 (6-10 weeks old, initial body weight 20-31 g)[1]
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Dosage:30 mg/kg (single-agent); 30 mg/kg (combination with 60 mg/kg Adavosertib)
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Administration:i.p.; daily; 21 days
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Result:Showed slightly better quantitative control of tumor growth versus VIC-1911 as a single agent, but this did not reach statistical significance.
Provided good tumor growth control when used in combination with adavosertib.
Caused no significant changes in body weight in any treatment group.
Chemical Information
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Masse moléculaire 1128.05
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Formule C56H60Cl2F4N12O5
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SMILES
NC(C1=C(NC2=CC=C(N3CCN(C(CCCCCNC(C4(CC5=NC(NC6=NNC(C)=C6)=C(F)C=C5)CCN(C(C7=C(Cl)C(Cl)=CC=C7)=O)CC4)=O)=O)CC3)C=C2)C=C(N8C(CC(C)(C)CC9=O)=C9C(C(F)(F)F)=N8)C=C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NN-01-195 Related Classifications
HY-181626 Related Classifications
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