Cat. No.: HY-50673

Dactolisib

(Synonyms: BEZ235; NVP-BEZ235)

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Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC₅₀s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.

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Pureté: 99.94%
CAS No.: 915019-65-7
Formule: C₃₀H₂₃N₅O
Masse moléculaire:469.54

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Dactolisib Chemical Structure

CAS No.: 915019-65-7

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (71)
Solvant et solubilité
- In Vitro
- In Vivo
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Pureté et documentation
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Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

p110α

4 nM (IC₅₀)

p110α-H1047R

4.6 nM (IC₅₀)

p110α-E545K

5.7 nM (IC₅₀)

p110γ

5 nM (IC₅₀)

p110δ

7 nM (IC₅₀)

p110β

75 nM (IC₅₀)

mTOR

20.7 nM (IC₅₀)

mTORC1

mTORC2

Autophagy

Voir tous les produits spécifiques à Isoform PI3K :

Voir tous les produits spécifiques à Isoform mTOR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.58 μM Compound: BEZ235	Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
A-431	IC₅₀	12.5 μM Compound: BEZ-235	Cytotoxicity against human A431 cells after 24 hrs by MTT assay Cytotoxicity against human A431 cells after 24 hrs by MTT assay	[PMID: 25062005]
A549	IC₅₀	0.1 μM Compound: BEZ235	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 24878359]
A549	IC₅₀	0.28 μM Compound: BEZ235	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26210161]
A549	IC₅₀	0.38 μM Compound: BEZ235	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
A549	IC₅₀	0.62 μM Compound: BEZ235	Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
A549	IC₅₀	0.62 μM Compound: Dactolisib	Cytotoxicity against human A549 cells after 72 hrs by SRB assay Cytotoxicity against human A549 cells after 72 hrs by SRB assay	[PMID: 29407971]
A549	IC₅₀	0.76 μM Compound: BEZ235	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
A549	IC₅₀	1.08 μM Compound: BEZ235	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
A549	IC₅₀	6.5 μM Compound: BEZ-235	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 25062005]
A549	IC₅₀	6.5 μM Compound: BEZ-235	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 25088398]
BT-549	IC₅₀	0.74 μM Compound: Dactolisib	Cytotoxicity against human BT549 cells after 72 hrs by SRB assay Cytotoxicity against human BT549 cells after 72 hrs by SRB assay	[PMID: 29407971]
COLO 205	IC₅₀	0.085 μM Compound: BEZ-235	Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay	[PMID: 25062005]
COLO 205	IC₅₀	0.085 μM Compound: BEZ-235	Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay	[PMID: 25088398]
EOL1	IC₅₀	1.05 μM Compound: Dactolisib	Antiproliferative activity against human EOL1 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human EOL1 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
HCC827	IC₅₀	0.53 μM Compound: BEZ235	Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis	[PMID: 34403956]
HCT-116	IC₅₀	0.044 μM Compound: BEZ-235	Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay	[PMID: 25062005]
HCT-116	IC₅₀	0.044 μM Compound: BEZ-235	Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 25088398]
HCT-116	IC₅₀	0.14 μM Compound: 1; BEZ-235	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	10.1039/C5MD00401B
HCT-116	IC₅₀	0.2 μM Compound: BEZ-235	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 26596710]
HCT-116	IC₅₀	0.22 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 28109945]
HCT-116	IC₅₀	0.24 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
HCT-116	IC₅₀	0.29 μM Compound: BEZ235	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26210161]
HCT-116	IC₅₀	0.29 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
HCT-116	IC₅₀	0.3 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 31434616]
HCT-116	IC₅₀	0.32 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 24878359]
HCT-116	IC₅₀	0.37 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay	[PMID: 27544401]
HCT-116	IC₅₀	0.37 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells harboring PIK3CA mutant H1047R measured after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells harboring PIK3CA mutant H1047R measured after 72 hrs by MTT assay	[PMID: 31176568]
HCT-116	IC₅₀	0.56 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay	[PMID: 26652969]
HCT-116	IC₅₀	0.84 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
HCT-116	IC₅₀	0.84 μM Compound: Dactolisib	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 29407971]
HCT-116	IC₅₀	0.84 μM Compound: Dactolisib	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 29937355]
HCT-116	IC₅₀	1.16 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 23871904]
HCT-116	IC₅₀	1.7 μM Compound: BEZ235	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HCT-15	IC₅₀	0.91 μM Compound: BEZ235	Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HEK-293T	CC₅₀	>5 μM Compound: 60; BEZ-235	Cytotoxicity against HEK293T cells Cytotoxicity against HEK293T cells	[PMID: 33539089]
HEL	IC₅₀	0.29 μM Compound: BEZ235	Antiproliferative activity against human HEL cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis Antiproliferative activity against human HEL cells assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis	[PMID: 34403956]
HeLa	IC₅₀	1.09 μM Compound: BEZ235	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HeLa	IC₅₀	1.17 μM Compound: BEZ235	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HepG2	IC₅₀	4.04 μM Compound: BEZ235	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HL-60	IC₅₀	0.51 μM Compound: Dactolisib	Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
HL-60	IC₅₀	0.91 μM Compound: BEZ235	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
HL-60	IC₅₀	1 μM Compound: 5; BEZ235	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 30077608]
HL-60	IC₅₀	12.42 μM Compound: BEZ-235	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 25088398]
HT-29	IC₅₀	1.01 μM Compound: BEZ235	Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
Huh-7	IC₅₀	0.53 μM Compound: BEZ235	Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
K562	ED₅₀	0.02021 μM Compound: 3; BEZ-235	Potentiation of (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as (-)-lomaiviticin A ED50 at compound to (-)-lomaiviticin A ratio of 200:1 after 48 hrs by cell titer-glo luminescence assay (Rvb = 0.23776 nM) Potentiation of (-)-lomaiviticin A-induced cytotoxicity against human K562 cells assessed as (-)-lomaiviticin A ED50 at compound to (-)-lomaiviticin A ratio of 200:1 after 48 hrs by cell titer-glo luminescence assay (Rvb = 0.23776 nM)	[PMID: 27177826]
K562	ED₅₀	0.04893 μM Compound: 3; BEZ-235	Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by cell titer-glo luminescence assay	[PMID: 27177826]
K562	IC₅₀	5.7 μM Compound: 5; BEZ235	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 30077608]
KG-1	IC₅₀	1.31 μM Compound: Dactolisib	Antiproliferative activity against human KG-1 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human KG-1 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
MCF7	GI₅₀	0.06 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human MCF7 cells after 72 hrs by SRB assay Growth inhibition of human MCF7 cells after 72 hrs by SRB assay	[PMID: 28835805]
MCF7	IC₅₀	0.05 μM Compound: 1; BEZ-235	Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay	10.1039/C5MD00401B
MCF7	IC₅₀	0.05 μM Compound: BEZ-235	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 26596710]
MCF7	IC₅₀	0.2 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31434616]
MCF7	IC₅₀	0.26 μM Compound: BEZ235	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26210161]
MCF7	IC₅₀	0.35 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay	[PMID: 27544401]
MCF7	IC₅₀	0.35 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells harboring PIK3CA mutant E545K measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PIK3CA mutant E545K measured after 72 hrs by MTT assay	[PMID: 31176568]
MCF7	IC₅₀	0.45 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
MCF7	IC₅₀	0.48 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
MCF7	IC₅₀	0.55 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 24878359]
MCF7	IC₅₀	0.73 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23871904]
MCF7	IC₅₀	1.09 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PI3CA E545K mutant after 72 hrs by MTT assay	[PMID: 26652969]
MCF7	IC₅₀	1.33 μM Compound: BEZ235	Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
MCF7	IC₅₀	1.33 μM Compound: Dactolisib	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 29407971]
MDA-MB-231	IC₅₀	0.18 μM Compound: BEZ235	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
MDA-MB-231	IC₅₀	0.56 μM Compound: Dactolisib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 29937355]
MOLM-16	IC₅₀	0.5 μM Compound: Dactolisib	Antiproliferative activity against human MOLM16 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MOLM16 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
MV4-11	IC₅₀	0.03 μM Compound: Dactolisib	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay	[PMID: 37329712]
NCI-H23	IC₅₀	1 μM Compound: BEZ235	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
NCI-H3122	IC₅₀	0.96 μM Compound: BEZ235	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H446	IC₅₀	0.87 μM Compound: BEZ235	Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H460	GI₅₀	0.61 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay Growth inhibition of human NCI-H460 cells after 72 hrs by SRB assay	[PMID: 28835805]
PC-3	IC₅₀	0.19 μM Compound: 1; BEZ-235	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay	10.1039/C5MD00401B
PC-3	IC₅₀	0.21 μM Compound: BEZ-235	Cytotoxicity against human PC3 cells after 72 hrs by SRB assay Cytotoxicity against human PC3 cells after 72 hrs by SRB assay	[PMID: 26596710]
PC-3	IC₅₀	0.51 μM Compound: BEZ235	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay	[PMID: 28109945]
PC-3	IC₅₀	12.3 μM Compound: BEZ-235	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay Cytotoxicity against human PC3 cells after 24 hrs by MTT assay	[PMID: 25062005]
PC-3	IC₅₀	12.3 μM Compound: BEZ-235	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 25088398]
Raji	IC₅₀	0.22 μM Compound: 4; BEZ235	Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Raji	IC₅₀	0.3 μM Compound: BEZ235	Antiproliferative activity against human Raji cells assessed as inhibition of cell growth after 48 hrs by MTT assay Antiproliferative activity against human Raji cells assessed as inhibition of cell growth after 48 hrs by MTT assay	[PMID: 32987316]
Raji	IC₅₀	0.52 μM Compound: BEZ235	Antiproliferative activity against human Raji cells by MTT assay Antiproliferative activity against human Raji cells by MTT assay	[PMID: 31434616]
Raji	IC₅₀	4.3 μM Compound: 5; BEZ235	Antiproliferative activity against human Raji cells after 48 hrs by MTT assay Antiproliferative activity against human Raji cells after 48 hrs by MTT assay	[PMID: 30077608]
Ramos	IC₅₀	0.0068 μM Compound: 4; BEZ235	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Ramos	IC₅₀	0.4 μM Compound: BEZ235	Antiproliferative activity against human Ramos cells by MTT assay Antiproliferative activity against human Ramos cells by MTT assay	[PMID: 31434616]
Ramos	IC₅₀	0.6 μM Compound: BEZ235	Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth after 48 hrs by MTT assay Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth after 48 hrs by MTT assay	[PMID: 32987316]
SH-SY5Y	IC₅₀	0.79 μM Compound: BEZ235	Antiproliferative activity against human SH-SY5Y assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis Antiproliferative activity against human SH-SY5Y assessed as reduction in cell viability measured after 72 hrs by flow cytometry analysis	[PMID: 34403956]
SK-HEP1	IC₅₀	1.82 μM Compound: BEZ235	Antiproliferative activity against human SKHEP1 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human SKHEP1 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
SK-HEP1	IC₅₀	1.82 μM Compound: Dactolisib	Cytotoxicity against human SKHEP1 cells after 72 hrs by SRB assay Cytotoxicity against human SKHEP1 cells after 72 hrs by SRB assay	[PMID: 29407971]
SNU-638	IC₅₀	1.24 μM Compound: BEZ235	Antiproliferative activity against human SNU638 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human SNU638 cells after 72 hrs by sulforhodamine B assay	[PMID: 29475582]
SNU-638	IC₅₀	1.24 μM Compound: Dactolisib	Cytotoxicity against human SNU638 cells after 72 hrs by SRB assay Cytotoxicity against human SNU638 cells after 72 hrs by SRB assay	[PMID: 29407971]
SNU-638	IC₅₀	1.24 μM Compound: Dactolisib	Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay	[PMID: 29937355]
SU-DHL-6	IC₅₀	0.07 μM Compound: BEZ235	Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by CCK-8 assay	[PMID: 31176568]
SW-620	IC₅₀	0.87 μM Compound: BEZ235	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
T47D	GI₅₀	0.3 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human T47D cells after 72 hrs by SRB assay Growth inhibition of human T47D cells after 72 hrs by SRB assay	[PMID: 28835805]
T47D	IC₅₀	11.2 μM Compound: BEZ-235	Cytotoxicity against human T47D cells after 24 hrs by MTT assay Cytotoxicity against human T47D cells after 24 hrs by MTT assay	[PMID: 25062005]
U-87MG ATCC	GI₅₀	0.28 μM Compound: NVP-BEZ235; BEZ235	Growth inhibition of human U87MG cells after 72 hrs by SRB assay Growth inhibition of human U87MG cells after 72 hrs by SRB assay	[PMID: 28835805]
U-87MG ATCC	IC₅₀	0.16 μM Compound: NVP-BEZ235	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 72 hrs by Z2 coulter counter method Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 72 hrs by Z2 coulter counter method	[PMID: 27081742]
U-87MG ATCC	IC₅₀	0.6 μM Compound: NVP-BEZ235	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs by Z2 coulter counter method Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 48 hrs by Z2 coulter counter method	[PMID: 27081742]
U-87MG ATCC	IC₅₀	0.77 μM Compound: BEZ235	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 26210161]
U-87MG ATCC	IC₅₀	1.32 μM Compound: BEZ235	Antiproliferative activity against human U87MG cells after 48 hrs by MTT assay Antiproliferative activity against human U87MG cells after 48 hrs by MTT assay	[PMID: 23871904]
U-87MG ATCC	IC₅₀	1.41 μM Compound: BEZ235	Antiproliferative activity against human U87MG cells incubated for 72 hrs by MTT assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
U-87MG ATCC	IC₅₀	2.34 μM Compound: BEZ235	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 24878359]
U-87MG ATCC	IC₅₀	824.7 μM Compound: NVP-BEZ235	Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 24 hrs by Z2 coulter counter method Cytotoxicity against human U87MG cells assessed as reduction in cell viability after 24 hrs by Z2 coulter counter method	[PMID: 27081742]

In Vitro

Dactolisib (BEZ235) potently inhibits PI3K in an ATP Competitive Manner. Dactolisib (BEZ235) (250 nM) significantly reduced the phosphorylation levels of the mTOR activated kinase p70S6K. Dactolisib (BEZ235) also leads to a reduction of S235/S236P-RPS6 levels with an IC₅₀ of 6.5 nM, suggesting that Dactolisib (BEZ235) can directly inhibit the mTOR kinase, as the kinase domain of mTOR is highly homologous to the one of class IA PI3K. The activity of Dactolisib (BEZ235) against mTOR is confirmed using a biochemical mTOR K-LISA assay (IC₅₀, 20.7 nM)^[1].
The IC₅₀s of Dactolisib (BEZ235) for HCT116, DLD-1, and SW480 cell lines are 14.3±6.4, 9.0±1.5, and 12.0±1.6 nM, respectively^[2].

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

In Vivo

Dactolisib (BEZ235) (45 mg/kg, p.o.) treatment induces colonic tumor regression in a GEM model for sporadic PIK3CA wild-type CRC^[2]. Dactolisib (BEZ235) (45 mg/kg) is administered to MENX rats (n=2 each group) by oral gavage and animals are sacrificed 1 or 6 hours after treatment. Immunostains for P-AKT and P-S6 show considerable reduction of the two proteins, and particularly of P-S6, 6 hours after administration of Dactolisib (BEZ235) when compares with PEG-treated rats. At 6 hours after treatment, the pituitary adenomas of Dactolisib (BEZ235)-treated rats has a proteomic profile significantly different from the tumors of placebo-treated rats^[3].

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

Chemical Information

CAS No. 915019-65-7
Appearance Solid
Masse moléculaire 469.54
Formule C₃₀H₂₃N₅O
Color White to light yellow
SMILES

CN(C1=C2C3=CC(C4=CC5=CC=CC=C5N=C4)=CC=C3N=C1)C(N2C6=CC=C(C=C6)C(C)(C#N)C)=O
Synonyms

BEZ235; NVP-BEZ235
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (71)

All WB

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Nature

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors. [Abstract]

2018 Aug;560(7719):499-503. PMID: 30051890
Cell

Innate immune and metabolic signals induce mitochondria-dependent membrane lysis via mitoxyperiosis. [Abstract]

2025 Dec 11;188(25):7155-7174.e25. PMID: 41317732
Cell Res

Endothelial CDS2 deficiency causes VEGFA-mediated vascular regression and tumor inhibition. [Abstract]

2019 Nov;29(11):895-910. PMID: 31501519
Blood

Suz12 inactivation cooperates with JAK3 mutant signaling in the development of T-cell acute lymphoblastic leukemia. [Abstract]

2019 Oct 17;134(16):1323-1336. PMID: 31492675
Cancer Res

H4K20me3-Mediated Repression of Inflammatory Genes Is a Characteristic and Targetable Vulnerability of Persister Cancer Cells. [Abstract]

2025 Jan 2;85(1):32-51. PMID: 39476057
Nat Commun

Intrinsic resistance to RAS inhibitors is driven by dysregulation of KRAS degradation. [Abstract]

2025 Dec 15. PMID: 41397976
Nat Commun

Codon bias imposes a targetable limitation on KRAS-driven therapeutic resistance. [Abstract]

2017 Jun 8;8:15617. PMID: 28593995

Dactolisib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]

Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors BEZ235 (Dactolisib).
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

EETs Reduction Contributes to Granulosa Cell Senescence and Endometriosis-Associated Infertility via the PI3K/AKT/mTOR Signaling Pathway. [Abstract]

2025 Aug 19:e05656. PMID: 40827571
Adv Sci (Weinh)

ANO1-Mediated Inhibition of Cancer Ferroptosis Confers Immunotherapeutic Resistance through Recruiting Cancer-Associated Fibroblasts. [Abstract]

2023 Aug;10(24):e2300881. PMID: 37341301
Exp Hematol Oncol

Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]

2016 Jul 29:5:22. PMID: 27478685
Leukemia

BET inhibitor-based combinations targeting novel dependencies in MECOM-rearranged (r) AML. [Abstract]

2025 Dec 19. PMID: 41419608
Leukemia

Repression of BIM mediates survival signaling by MYC and AKT in high-risk T-cell acute lymphoblastic leukemia. [Abstract]

2014 Sep;28(9):1819-27. PMID: 24552990

Dactolisib purchased from MedChemExpress. Usage Cited in: Leukemia. 2014 Sep;28(9):1819-27. [Abstract]

Western blot analysis of human T-ALL cell lines treated for 24 hours using DMSO (vehicle control), 1 μM JQ1, 500 nM BEZ235, or both drugs in combination, using the indicated antibodies. Western blot analysis of these T-ALL cell lines following treatment with JQ1, BEZ235 or both drugs in combination reveals cooperative upregulation of BIM protein expression coupled to induction of apoptosis, as assessed by PARP cleavage.
J Exp Clin Cancer Res

TSSC3 promotes autophagy via inactivating the Src-mediated PI3K/Akt/mTOR pathway to suppress tumorigenesis and metastasis in osteosarcoma, and predicts a favorable prognosis. [Abstract]

2018 Aug 9;37(1):188. PMID: 30092789

Dactolisib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 9;37(1):188. [Abstract]

Representative images of the western blotting analysis of TSSC3, ATG5, P62, LC3, Src, Akt, mTOR and their phosphorylated versions in MTF and SaOS2 cells. Cells are treated with TSSC3-overexpression, IGF-1, p-YEEI, and BEZ235 separately or in combination.
J Nanobiotechnology

Carbonic anhydrase IX-targeted H-APBC nanosystem combined with phototherapy facilitates the efficacy of PI3K/mTOR inhibitor and resists HIF-1α-dependent tumor hypoxia adaptation. [Abstract]

2022 Apr 12;20(1):187. PMID: 35413842
Sci Adv

Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding. [Abstract]

2023 Mar 22;9(12):eadd5028. PMID: 36947620
EBioMedicine

PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. [Abstract]

2015 Nov 19;2(12):1944-56. PMID: 26844273
Cell Death Dis

Pictilisib and nutrient stress synergize to induce methuosis via PI(4,5)P2-dependent macropinocytic dysregulation in cancer cells. [Abstract]

2026 Jun 16. PMID: 42303628
Cell Death Dis

A novel 4-aminoquinazoline derivative, DHW-208, suppresses the growth of human breast cancer cells by targeting the PI3K/AKT/mTOR pathway. [Abstract]

2020 Jun 30;11(6):491. PMID: 32606352
Cell Commun Signal

Autophagy modulators influence the content of important signalling molecules in PS-positive extracellular vesicles. [Abstract]

2023 May 24;21(1):120. PMID: 37226246
BMC Med

HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]

2021 Oct 15;19(1):247. PMID: 34649530
NPJ Precis Oncol

Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]

2025 Nov 21;9(1):373. PMID: 41272086
Haematologica

Human BCR/ABL1 induces chronic myeloid leukemia-like disease in zebrafish. [Abstract]

2020 Mar;105(3):674-686. PMID: 31289206
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Br J Cancer

METTL14-mediated N6-methyladenosine modification of Pten mRNA inhibits tumour progression in clear-cell renal cell carcinoma. [Abstract]

2022 Jul;127(1):30-42. PMID: 35249103
Sci Signal

TSHZ2 is an EGF-regulated tumor suppressor that binds to the cytokinesis regulator PRC1 and inhibits metastasis. [Abstract]

2021 Jun 22;14(688):eabe6156. PMID: 34158398
JCI Insight

ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors. [Abstract]

2022 Aug 22;7(16):e155899. PMID: 35852858
Cancer Cell Int

FAP promotes clear cell renal cell carcinoma progression via activating the PI3K/AKT/mTOR signaling pathway. [Abstract]

2023 Sep 27;23(1):217. PMID: 37752545
Eur J Med Chem

Discovery of N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia. [Abstract]

2023 Oct 5:258:115543. PMID: 37329712
Biochem Pharmacol

DZW-310, a novel phosphoinositide 3-kinase inhibitor, attenuates the angiogenesis and growth of hepatocellular carcinoma cells via PI3K/AKT/mTOR axis. [Abstract]

2022 Jul:201:115093. PMID: 35580648
Mol Cancer Ther

A Novel Combination Approach Targeting an Enhanced Protein Synthesis Pathway in MYC-driven (Group 3) Medulloblastoma. [Abstract]

2020 Jun;19(6):1351-1362. PMID: 32371591
Cancer Gene Ther

METTL3-mediated maturation of miR-126-5p promotes ovarian cancer progression via PTEN-mediated PI3K/Akt/mTOR pathway. [Abstract]

2021 Apr;28(3-4):335-349. PMID: 32939058
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
J Mol Cell Cardiol

MicroRNA-223 protects neonatal rat cardiomyocytes and H9c2 cells from hypoxia-induced apoptosis and excessive autophagy via the Akt/mTOR pathway by targeting PARP-1. [Abstract]

2018 May:118:133-146. PMID: 29608885
Molecules

A PI3K Inhibitor with Low Cardiotoxicity and Its Synergistic Inhibitory Effect with Gilteritinib in Acute Myelogenous Leukemia (AML) Cells. [Abstract]

2025 May 27;30(11):2347. PMID: 40509234
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Molecules

Screening of PI3K-Akt-targeting Drugs for Silkworm against Bombyx mori Nucleopolyhedrovirus. [Abstract]

2019 Apr 1;24(7):1260. PMID: 30939726
Cancers (Basel)

Early Mechanisms of Chemoresistance in Retinoblastoma. [Abstract]

2022 Oct 10;14(19):4966. PMID: 36230889
Sci Rep

Glutamine and serum starvation alters the ATP production, oxidative stress, and abundance of mitochondrial RNAs in extracellular vesicles produced by cancer cells. [Abstract]

2024 Oct 28;14(1):25815. PMID: 39468126
J Biol Chem

The mTOR inhibitor manassantin B reveals a crucial role of mTORC2 signaling in Epstein-Barr virus reactivation. [Abstract]

2020 May 22;295(21):7431-7441. PMID: 32312752
Sci Rep

Drug-induced PD-L1 expression and cell stress response in breast cancer cells can be balanced by drug combination. [Abstract]

2019 Oct 22;9(1):15099. PMID: 31641154
Exp Mol Pathol

NVP-BEZ235 enhances autophagy and ameliorates cognitive deficits by targeting tauopathies. [Abstract]

2025 Jul 24:143:104988. PMID: 40712456
Cell Signal

MEK inhibitor trametinib combined with PI3K/mTOR inhibitor BEZ-235 as an effective strategy against NSCLC through impairment of glucose metabolism. [Abstract]

2024 Sep 16:111415. PMID: 39293743
Arch Pharm (Weinheim)

Discovery of potent CSK inhibitors through integrated virtual screening and molecular dynamic simulation. [Abstract]

2024 Sep;357(9):e2400066. PMID: 38809025
Front Oncol

FGF1 protects FGFR1-overexpressing cancer cells against drugs targeting tubulin polymerization by activating AKT via two independent mechanisms. [Abstract]

2022 Oct 6:12:1011762. PMID: 36276073
Int J Med Sci

Dual PI3K/mTOR Inhibitor BEZ235 combined with BMS-1166 Promoting Apoptosis in Colorectal Cancer. [Abstract]

2024 Jul 9;21(10):1814-1823. PMID: 39113885
Anim Cells Syst

UCH-L1 and UCH-L3 regulate the cancer stem cell-like properties through PI3 K/Akt signaling pathway in prostate cancer cells. [Abstract]

2021 Oct 11;25(5):312-322. PMID: 34745437
Kaohsiung J Med Sci

WDR72 Drives Esophageal Squamous Cell Carcinoma Progression by Inhibiting Autophagy via the PI3K/Akt/mTOR Pathway. [Abstract]

2026 Jun 1:e70235. PMID: 42224092
J Orthop Surg Res

Epimedium Brevicornu and Curculigo orchioides inhibit osteoclast autophagy by degrading the level of miRNA-199 to regulate the mTOR signaling pathway. [Abstract]

2025 Jul 9;20(1):631. PMID: 40635043
Oncotargets Ther

The Immunostimulative Effect and Mechanisms of a Novel Mouse Anti-Human PD-1 Monoclonal Antibody on Jurkat Lymphocytic Cells Cocultured with Hepatoma Cells. [Abstract]

2020 Nov 27;13:12225-12241. PMID: 33273828
Onco Targets Ther

FNDC3B, Targeted by miR-125a-5p and miR-217, Promotes the Proliferation and Invasion of Colorectal Cancer Cells via PI3K/mTOR Signaling. [Abstract]

2020 Apr 30;13:3501-3510. PMID: 32431508
Gene

Epigenetic activation of PTEN by valproic acid inhibits PI3K/AKT signaling and Burkitt lymphoma cell growth. [Abstract]

2025 May 20:950:149369. PMID: 40021103
Biomed Res Int

BEZ235 Increases the Sensitivity of Hepatocellular Carcinoma to Sorafenib by Inhibiting PI3K/AKT/mTOR and Inducing Autophagy. [Abstract]

2021 Apr 16:2021:5556306. PMID: 33987439
Biomed Res Int

Study on Biological Characteristics and Mechanism of Paclitaxel Induced Drug Resistance in Endometrial Carcinoma Cells. [Abstract]

2018 Aug 5:2018:8372085. PMID: 30175145

Dactolisib purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2018 Aug 5:2018:8372085. [Abstract]

Changes of p-AKT and p-p70 S6K proteins after treatment with NVP-BEZ235 in Ishikawa and Ishikawa-TAX cells. Changes of p-AKT and p-p70 S6K proteins after treatment of Ishikawa and Ishikawa-TAX cells with NVP-BEZ235.
J Chemother

BEZ235 reduction of cisplatin resistance on wild-type EGFR non-small cell lung cancer cells. [Abstract]

2023 Apr;35(2):95-103. PMID: 35238281
Am J Transl Res

BEZ235 increases sorafenib inhibition of hepatocellular carcinoma cells by suppressing the PI3K/AKT/mTOR pathway. [Abstract]

2019 Sep 15;11(9):5573-5585. PMID: 31632530
bioRxiv

2026 Jun 7.
Res Sq

2026 Jan 9.
Patent

US20210236501A1.
Actome

2024.
bioRxiv

2024 September 10.
Oxid Med Cell Longev

SPP1 Promotes Enzalutamide Resistance and Epithelial-Mesenchymal-Transition Activation in Castration-Resistant Prostate Cancer via PI3K/AKT and ERK1/2 Pathways. [Abstract]

2021 Oct 22:2021:5806602. PMID: 34721759
University of North Carolina

2021.
Oncotarget

Oridonin inhibits aberrant AKT activation in breast cancer. [Abstract]

2018 Feb 1;9(35):23878-23889. PMID: 29844859
Oncotarget

The effect of rapamycin, NVP-BEZ235, aspirin, and metformin on PI3K/AKT/mTOR signaling pathway of PIK3CA-related overgrowth spectrum (PROS). [Abstract]

2017 Jul 11;8(28):45470-45483. PMID: 28525374

Dactolisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 11;8(28):45470-45483. [Abstract]

Activity of PI3K/AKT/mTOR is monitored by examining phosphorylation of AKT-S473, AKT-T308, and S6 by western blotting.
Am J Dig Dis (Madison)

2015;2(2):95-99.
J Clin Toxicol

2014 October 4, 4:5.
J Clin Toxicol 2014, 4:5

Solvant et solubilité

In Vitro:

5% TFA : 8.33 mg/mL (17.74 mM; ultrasonic and warming and heat to 60°C)

DMF : 2 mg/mL (4.26 mM; Need ultrasonic)

DMSO : 1 mg/mL (2.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1297 mL

10.6487 mL

21.2974 mL

5 mM

0.4259 mL

2.1297 mL

4.2595 mL

10 mM

0.2130 mL

1.0649 mL

2.1297 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.52 mg/mL (1.11 mM); Clear solution

This protocol yields a clear solution of ≥ 0.52 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.52 mg/mL (1.11 mM); Clear solution

This protocol yields a clear solution of ≥ 0.52 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.2 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 12.5 mg/mL (26.62 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 10% 1-Methyl-2-pyrrolidinone 90% PEG300

Solubility: ≥ 1.1 mg/mL (2.34 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[2]

HCT116 (PIK3CA mutant; kinase domain at H1047R), DLD-1 (PIK3CA mutant; helical domain at E545K), and SW480 (PIK3CA wild-type) human CRC cell lines (ATCC) and isogenic DLD-1 PIK3CA mutant and wild-type cells are maintained in DMEM. Cells are plated at different initial densities (HCT116: 3,000 cells/well, DLD-1: 5,500 cells/well, SW480: 4,500 cells/well, DLD-1 PIK3CA mutant: 7,000 cells/well, and DLD-1 PIK3CA wild-type: 9,000 cells/well) to account for differential growth kinetics. After 16 hours, cells are incubated with increasing concentrations of BEZ235 (10, 100, 1000 nM), and drug-containing growth medium is changed every 24 hours. Cell viability is assessed 16 hours after the initial plating and 48 hours after initiation of drug treatment using the colorimetric MTS assay CellTiter 96 AQueous One Solution Cell Proliferation Assay. Cell viability after drug treatment is normalized to that of untreated cells also grown for 48 hours. IC₅₀ values are calculated using 4 parameter nonlinear regression in GraphPad Prism 5^[2].

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

Animal Administration^[2]^[3]

Mice^[2]
Tumor-bearing Apc CKO mice are randomly assigned to treatment with either control vehicle alone (n=8) or 45 mg/kg body weight BEZ235 in 10% 1-methyl-2-pyrrolidone/90% PEG 300 (n=8) by daily oral gavage for 28 days. The treatment dose is chosen based on literature indicating that 40-50 mg/kg body weight BEZ235 effectively treats murine tumor models without adverse effects. Base on pharmacokinetic studies demonstrating maximal tissue concentration one hour after NVP-BEZ235 administration, tumor-bearing mice are sacrificed one hour after final treatment dose. Colonic tumor volume is assessed using calipers (width×length×height) and tumors are harvested for both western blot analysis and immunohistochemistry.
Rats^[3]
MENX-affected rats used. Three doses of BEZ235 are tested in MENX rats: 20, 30, and 45 mg/kg. As the two higher doses causes a weight loss >10% after 10 days of treatment, the dose of 20 mg/kg is used for further studies. For MRI studies, MENX-affected rats at 7 to 8 months of age (with sizeable adenomas but still in good general health) are treated for 14 days with BEZ235 (20 mg/kg) or placebo (PEG) administered daily per oral gavage.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (287 KB)
SDS (396 KB)
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Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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Références

[1]. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863. [Content Brief]

[2]. Roper J, et al. The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer. PLoS One, 2011, 6(9), e25132. [Content Brief]

[3]. Lee M, et al. Targeting PI3K/mTOR Signaling Displays Potent Antitumor Efficacy against Nonfunctioning Pituitary Adenomas. Clin Cancer Res. 2015 Jul 15;21(14):3204-15. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / DMF / 5% TFA	1 mM	2.1297 mL	10.6487 mL	21.2974 mL	53.2436 mL
5% TFA	5 mM	0.4259 mL	2.1297 mL	4.2595 mL	10.6487 mL
	10 mM	0.2130 mL	1.0649 mL	2.1297 mL	5.3244 mL
	15 mM	0.1420 mL	0.7099 mL	1.4198 mL	3.5496 mL

Keywords

Dactolisib

71 Cited Publications

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Dactolisib

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Voir tous les produits spécifiques à Isoform PI3K

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Activité biologique

Chemical Information

Publications (71)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Dactolisib

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Dactolisib

Voir tous les produits spécifiques à Isoform PI3K

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Activité biologique

Chemical Information

Publications (71)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Dactolisib Related Classifications

HY-50673 Related Classifications