BEZ235 (NVP-BEZ235, Dactolisib)

Catalog No. A10133

BEZ235 (NVP-BEZ235,Dactolisib)是通过与这些酶的ATP结合裂隙结合来抑制PI3K和mTOR激酶活性。

Product Citations

Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902

Technical details

Catalog Num	A10133
M. Wt	469.6
Formula	C30H23N5O
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	915019-65-7
Synonyms
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

Biological Activity

BEZ235 (NVP-BEZ235,Dactolisib)是通过与这些酶的ATP结合裂隙结合来抑制PI3K和mTOR激酶活性。

Targets

Target	Value
p110α	IC50: 4nM
p110γ	IC50: 5nM
mTOR(p70S6K)	IC50: 6nM
p110δ	IC50: 7nM
ATR	IC50: 21nM
p110β	IC50: 75nM
EGFR/ErbB1	IC50: >8.5μM
VEGFR1/FLT1	IC50: >10μM
FLT3	IC50: >10μM
IGF-1R	IC50: >10μM
EphB4	IC50: >10μM
RET	IC50: >10μM
Tie-2	IC50: >10μM
c-Met	IC50: >10μM
FGFR(K650E)	IC50: >10μM
FAK	IC50: >10μM
JAK2	IC50: >10μM
c-Abl	IC50: >10μM
c-Src	IC50: >10μM
PKA	IC50: >10μM
Akt1/PKBα	IC50: >10μM
PDK-1	IC50: >10μM
B-Raf(V599E)	IC50: >10μM
CDK1	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	<1 mg/mL
	Water	Insoluble
	Ethanol	Warmed: 16 mg/mL (34.07 mM)
In vivo	NMP+PEG300 (10+90, v+v)	28 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	21.29 mL	106.47 mL	212.95 mL
0.5 mM	4.26 mL	21.29 mL	42.59 mL
1 mM	2.13 mL	10.65 mL	21.29 mL
5 mM	0.43 mL	2.13 mL	4.26 mL

*The above data is based on the productmolecular weight 469.6. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.