2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Epigenetics Apoptosis
  3. HSP Aurora Kinase Apoptosis
  4. NN-01-195

NN-01-195 is a HSP90 inhibitor-drug conjugate. 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.

For research use only. We do not sell to patients.

NN-01-195

NN-01-195 Chemical Structure

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NN-01-195 Related Antibodies

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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Description

NN-01-195 is a HSP90 inhibitor-drug conjugate. 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[1].

IC50 & Target[1]

HSP90α

8.7 nM (IC50)

In Vitro

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.

NN-01-195 Related Antibodies

Western Blot Analysis[1]

Cell Line: FaDu, NCI-H1975
Concentration: 500 and 1000 nM
Incubation Time: 72 h (cleaved PARP); 24 h (other targets)
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.
Parmacokinetics
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
In Vivo

NN-01-195 (10-80 mg/kg; i.p.; daily; 5 days) is well tolerated in C57BL/6J mice, with the highest dose of 80 mg/kg administered via daily intraperitoneal injection for 5 consecutive days causing no significant systemic toxicity[1].
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.

Animal Model: NSG treated FaDu (6-10 weeks old, initial body weight 20-31 g)[1]
Dosage: 30 mg/kg (single-agent); 30 mg/kg (combination with 60 mg/kg adavosertib)
Administration: i.p.; daily; 14 days
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.
Animal Model: NSG treate H1975 (6-10 weeks old, initial body weight 20-31 g)[1]
Dosage: 30 mg/kg (single-agent); 30 mg/kg (combination with 60 mg/kg Adavosertib)
Administration: i.p.; daily; 21 days
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.
Molecular Weight

1128.05

Formula

C56H60Cl2F4N12O5
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NN-01-195 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NN-01-195HSPAurora KinaseApoptosisHeat shock proteinsnon-small cell lung carcinomahead and neck squamous cell carcinomaNCI-H1975 non-small cell lung carcinoma cellsHSP90MRC5 fibroblastsHEK293T cellsmelanomasolid tumorsInhibitorinhibitorinhibit

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