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Merck
CN

444966

PD 0325901

≥95% (HPLC), MEK/MAPKK/MKK inhibitor, solid

别名:

MEK1/2抑制剂III

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关于此项目

经验公式（希尔记法）:
C16H14F3IN2O4
化学文摘社编号:
391210-10-9
分子量:
482.19
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD08435926
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze
protect from light

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产品名称

MEK1/2抑制剂III, The MEK1/2 Inhibitor III, also referenced under CAS 391210-10-9, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

Ic1cc(c(cc1)Nc2c(c(ccc2C(=O)NOC[C@H](O)CO)F)F)F

InChI

1S/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1

InChI key

SUDAHWBOROXANE-SECBINFHSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white to off-white

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

相关类别

Disclaimer

毒性：标准处理（A）

General description

一种可渗透细胞的苯甲酰胺化合物，可作为非竞争性，高效，选择性MEK/MAPKK/MKK抑制剂，并有效阻断细胞Erk1/2磷酸化（在血清刺激后血清饥饿的HeLa中降低>90%，在C26中降低50%，分别使用25和0.33 nM抑制剂），而在无细胞激酶测定中，即使在浓度为高10 µM的情况下，对Erk1/2或一组66种其他激酶的活性也影响很小或没有影响。显示可在小鼠中口服使用，并在体内抑制表达BRAF（V600E）的SKMEL28细胞源性肿瘤的生长和Erk磷酸化。也有InSolution 格式（目录号444968）。

Other Notes

Barrett, S.D., et al. 2008.Bioorg.Med. Chem. Lett.18, 6501.
Leyton, J., et al. 2008.Mol.Cancer Ther.7, 3112.
Silva, J., et al. 2008.PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008.Nature453, 519.
Bain, J., et al. 2007.Biochem.J.408, 297.
Solit, D.B., et al. 2006.Nature439, 358.

Packaging

用惰性气体包装

Preparation Note

复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多3个月。

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

pictograms

Skull and crossbonesHealth hazard
GHS06,GHS08

signalword

Danger

Hazard Classifications

Acute Tox. 3 Oral - Aquatic Chronic 4 - STOT RE 2

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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