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BEZ235 (NVP-BEZ235, Dactolisib)

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PI3K/mTOR 抑制剂

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产品目录号: A10133

库存状态:中国现货中国现货

产品名 目录号 价格 数量
BEZ235 25mg A10133-25
¥ 300.00
BEZ235 50mg A10133-50
¥ 500.00
BEZ235 100mg A10133-100
¥ 800.00
BEZ235 200mg A10133-200
¥ 1,400.00

产品仅用于研究,不针对患者销售,望谅解.

产品简介

BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.

BEZ235 (NVP-BEZ235, Dactolisib)

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顾客使用 Adooq 产品发表的高质量科研文献
Adooq 顾客使用 BEZ235 (NVP-BEZ235, Dactolisib) 发表的文献 (2)
  • 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每1975 PMID: 27725902

Chemical Information

目录号 A10133
Mechanism of action Inhibitor
分子量 469.6
化学分子式 C30H23N5O
Solubility DMSO>7mg/mL Water<1mg/mL Ethanol<1mg/mL
纯度 >98%
储存方式 at -20°C 2 years
CAS No. 915019-65-7
Synonyms N/A
SMILES code 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
化学名称 2-Methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl]phenyl]propionitrile

生物活性

Description
BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
Targets
Target Value
p110αIC50: 4nM
p110γIC50: 5nM
mTOR(p70S6K)IC50: 6nM
p110δIC50: 7nM
ATRIC50: 21nM
p110βIC50: 75nM
EGFR/ErbB1IC50: >8.5μM
VEGFR1/FLT1IC50: >10μM
FLT3IC50: >10μM
IGF-1RIC50: >10μM
EphB4IC50: >10μM
RETIC50: >10μM
Tie-2IC50: >10μM
c-MetIC50: >10μM
FGFR(K650E)IC50: >10μM
FAKIC50: >10μM
JAK2IC50: >10μM
c-AblIC50: >10μM
c-SrcIC50: >10μM
PKAIC50: >10μM
Akt1/PKBαIC50: >10μM
PDK-1IC50: >10μM
B-Raf(V599E)IC50: >10μM
CDK1IC50: >10μM

溶解性

Solubility (25°C) * In vitro DMSO 0.01 mg/mL (<1 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo NMP/polyethylene glycol 300 (10/90, v/v) 30 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.

制备储备液

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 21.29 mL 106.47 mL 212.95mL
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.

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