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NVP-BBD130

NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor. NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

CAS No.: 853910-61-9
Formula: C₂₈H₂₁N₅O
Molecular Weight:443.50

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

NVP-BBD130 Chemical Structure

CAS No.: 853910-61-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor^[1]. NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

PI3K, mTOR^[1]

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
U-87MG ATCC	EC₅₀	13 nM Compound: 7	Antiproliferative activity against human U87MG cells Antiproliferative activity against human U87MG cells	[PMID: 18248814]
U-87MG ATCC	IC₅₀	33 nM Compound: 7	Inhibition of phosphorylation of T308-PKB in human U87MG cells by ELISA Inhibition of phosphorylation of T308-PKB in human U87MG cells by ELISA	[PMID: 18248814]

In Vitro

NVP-BBD130 (1 μM; 72 h) blocks proliferation of melanoma cells, arrests cell cycle at G1 phase in A2058 cells but not C32 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

Melanoma cells
Concentration:

1 μM
Incubation Time:

3 days
Result:

Showed a long-term effect on melanoma cell proliferation.

Western Blot Analysis^[1]

Cell Line:

A2058 and C32 cells
Concentration:

1 μM
Incubation Time:

0, 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h
Result:

Decreased phosphorylation of PKB/Akt, whereas the phosphorylation status of MAPK was not affected.
Down-regulated the expression of cyclin D1, induced p27^Kip1 expression in A2058 cells.

Cell Cycle Analysis^[1]

Cell Line:

A2058 cells
Concentration:

1 μM
Incubation Time:

3 days
Result:

Resulted in a complete arrest of most tumor cells in G1.

In Vivo

NVP-BBD130 (40 mg/kg; p.o.; daily for 2 weeks) efficiently attenuates tumor growth at primary and lymph node metastatic sites with no obvious toxicity, and is well tolerant in B16BL6 mouse melanoma model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL6 mice, syngeneic B16BL6 mouse melanoma model^[1]
Dosage:

40 mg/kg
Administration:

Oral administration, daily for 2 weeks
Result:

Reduced primary tumor size, showed a significant reduction in the size of the cervical lymph node metastasis.

Chemical Information

CAS No. 853910-61-9
Molecular Weight 443.50
Formula C₂₈H₂₁N₅O
SMILES

N#CC(C)(C)C1=CC=C(N2C(N(C)C3=CN=C4C=CC(C#CC5=CC=CN=C5)=CC4=C32)=O)C=C1
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Marone R, et al. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol Cancer Res. 2009 Apr;7(4):601-13. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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NVP-BBD130

All PI3K Isoforms

All mTOR Isoforms