生物活性

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

化学数据

目录号	A10133
作用机制	Inhibitor (抑制剂)
M. Wt	469.6
Formula	C30H23N5O
Purity	>99%
Storage	Store lyophilized at -20?C, keep desiccated. In lyophilized form, the chemical is stable for36 months. In solution, store at -20?C and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
CAS No.	915019-65-7
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

溶解度

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.

储备液配制

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.