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AB120882

NVP-BEZ235, PI3K and mTOR inhibitor

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MW 469.5 Da, Purity >98%. Potent, ATP-competitive Phosphatidylinositol 3-​kinase (PI3K) inhibitor (IC50 = 4, 5, 7 and 75 nM for PI3Kα, -γ, -δ, and -β respectively) and mTOR inhibitor. Able to directly induce G1 arrest and inhibit angiogenesis in vitro and potentiate the efficacy of other anticancer agents in vivo.

View Alternative Names

1-phosphatidylinositol 3-kinase, 5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha, 5-bisphosphate 3-kinase 110 kDa catalytic subunit beta, 5-bisphosphate 3-kinase 110 kDa catalytic subunit delta, 5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma, 5-bisphosphate 3-kinase catalytic subunit alpha isoform, 5-bisphosphate 3-kinase catalytic subunit beta isoform, 5-bisphosphate 3-kinase catalytic subunit delta isoform, 5-bisphosphate 3-kinase catalytic subunit gamma isoform, AI838772, APDS, AW493413, CLOVE, CWS5, DKFZp779K1237, FK506 binding protein 12 rapamycin associated protein 1, FK506 binding protein 12 rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, FLJ11090, FLJ44809, FRAP, FRAP1, FRAP2, GRB 1, IMD14, MCAP, MCM, MCMTC, MGC104252, MGC112732, MGC133043, MGC142161, MGC142163, MTOR_HUMAN, Mammalian target of rapamycin, Mechanistic target of rapamycin, NF-E2-related factor 2, NF2L2_HUMAN, NRF2, Nfe2l2, Nuclear factor, Nuclear factor (erythroid derived 2) like 2, Nuclear factor erythroid 2-related factor 2, Nuclear factor erythroid derived 2 like 2, OTTHUMP00000001983, OTTHUMP00000216901, OTTHUMP00000216904, PI 3 Kinase catalytic subunit alpha, PI 3 Kinase catalytic subunit gamma, PI3 kinase p110 subunit alpha, PI3 kinase p110 subunit beta, PI3 kinase p110 subunit delta, PI3 kinase p110 subunit gamma, PI3-kinase subunit alpha, PI3-kinase subunit beta, PI3-kinase subunit delta, PI3-kinase subunit gamma, PI3CG, PI3K, PI3K-alpha, PI3K-beta, PI3K-delta, PI3K-gamma, PI3KC A, PI3KCB, PIK3, PIK3C A, PIK3C1, PIK3R1, PK3CA_HUMAN, PK3CB_HUMAN, PK3CD_HUMAN, PK3CG_HUMAN, Phosphatidylinositol 3 kinase catalytic alpha polypeptide, Phosphatidylinositol 3 kinase catalytic 110 KD alpha, Phosphatidylinositol 3 kinase catalytic 110 kD gamma, Phosphatidylinositol 3 kinase catalytic beta polypeptide, Phosphatidylinositol 3 kinase catalytic delta polypeptide, Phosphatidylinositol 3 kinase gamma, p110 gamma, Phosphatidylinositol 3 kinase, catalytic, gamma polypeptide, Phosphatidylinositol 4 5 bisphosphate 3 kinase 110 kDa catalytic subunit beta, Phosphatidylinositol 4 5 bisphosphate 3 kinase 110 kDa catalytic subunit gamma, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit alpha, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit alpha isoform, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit beta isoform, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit delta isoform, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit gamma, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit gamma isoform, Phosphatidylinositol 4,5 bisphosphate 3 kinase 110 kDa catalytic subunit alpha, Phosphatidylinositol 4,5 bisphosphate 3 kinase 110 kDa catalytic subunit delta, Phosphatidylinositol 4,5 bisphosphate 3 kinase, catalytic subunit delta, Phosphatidylinositol-4, Phosphoinositide 3 kinase B, Phosphoinositide 3 kinase C, Phosphoinositide 3 kinase catalytic alpha polypeptide, Phosphoinositide 3 kinase catalytic beta polypeptide, Phosphoinositide 3 kinase catalytic delta polypeptide, Phosphoinositide 3 kinase gamma catalytic subunit, Phosphoinositide 3 kinase, catalytic, delta polypeptide variant p37delta, Phosphoinositide-3-kinase catalytic gamma polypeptide, Pik3cb, Pik3cd, Pik3cg, PtdIns 3 kinase p110, PtdIns-3-kinase subunit alpha, PtdIns-3-kinase subunit beta, PtdIns-3-kinase subunit delta, PtdIns-3-kinase subunit gamma, PtdIns-3-kinase subunit p110-alpha, PtdIns-3-kinase subunit p110-beta, PtdIns-3-kinase subunit p110-delta, PtdIns-3-kinase subunit p110-gamma, RAFT1, RAPT1, RP24-311F12.2, Rapamycin and FKBP12 target 1, Rapamycin associated protein FRAP2, Rapamycin target protein, Rapamycin target protein 1, SCAN1, Serine/threonine protein kinase PIK3CA, Serine/threonine protein kinase PIK3CG, Serine/threonine-protein kinase mTOR, TYDP, TYDP1_HUMAN, Tyr-DNA phosphodiesterase 1, Tyrosyl-DNA phosphodiesterase 1, caPI3K, dJ576K7.1 (FK506 binding protein 12 rapamycin associated protein 1), erythroid derived 2, like 2, nuclear factor erythroid 2 like 2, p110 BETA, p110 alpha, p110 gamma, p110D, p110delta, p110dp85a, p120-PI3K, p85-ALPHA

1 Images
Chemical Structure - NVP-BEZ235, PI3K and mTOR inhibitor (AB120882)
  • Chemical Structure

Lab

Chemical Structure - NVP-BEZ235, PI3K and mTOR inhibitor (AB120882)

2D chemical structure image of ab120882, NVP-BEZ235, PI3K and mTOR inhibitor

Key facts

CAS number

915019-65-7

Purity

>98%

Form

Solid

form

Molecular weight

469.5 Da

Molecular formula

C<sub>3</sub><sub>0</sub>H<sub>2</sub><sub>3</sub>N<sub>5</sub>O

PubChem

11977753

Nature

Synthetic

Biochemical name

Dactolisib

Biological description

Potent, ATP-competitive Phosphatidylinositol 3-​kinase (PI3K) inhibitor (IC50 = 4, 5, 7 and 75 nM for PI3Kα, -γ, -δ, and -β respectively) and mTOR inhibitor. Able to directly induce G1 arrest and inhibit angiogenesis in vitro and potentiate the efficacy of other anticancer agents in vivo.

Canonical smiles

CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5

InChi

InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3

InChiKey

JOGKUKXHTYWRGZ-UHFFFAOYSA-N

IUPAC Name

2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions
Handling instructions

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Refer to SDS for further information.

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The mTOR protein also known as mechanistic target of rapamycin is a serine/threonine kinase with a mass of approximately 289 kDa. It is part of the PI3K-related kinase family and is widely expressed in various tissues. mTOR acts as a central regulator of cell growth and metabolism in response to nutrient availability growth factors and cellular energy status. It typically functions in two distinct complexes called mTORC1 and mTORC2 each involved in different cellular processes.
Biological function summary

The multifaceted mTOR protein has important roles in cellular processes such as protein synthesis autophagy and lipid biosynthesis. It interacts with numerous cellular components and is an important part of the mTORC1 and mTORC2 complexes which have different regulatory roles. The mTOR in its complex forms regulates cellular metabolism and helps control the response to stress and nutrients playing a significant part in cellular homeostasis.

Pathways

The protein mTOR integrates signals from critical pathways like the PI3K/AKT/mTOR and MAPK/ERK pathways. It closely interacts with proteins such as AKT (protein kinase B) and p70S6 kinase which are significant in signaling cascades. These pathways are involved in cell survival and growth and mTOR's regulation of these processes highlights its importance in cellular physiology.

MTOR is implicated in cancer and metabolic disorders. Its dysregulation often leads to uncontrolled cell growth contributing to oncogenesis. Specific inhibitors like NVP-BEZ235 (dactolisib) target the PI3K/mTOR pathway showing potential in cancer therapy. Additionally alterations in mTOR signaling are associated with metabolic diseases linking with proteins such as p110 beta and p110 delta which are PI3K isoforms involved in oncogenic and metabolic signaling pathways.

Product protocols

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