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Merck
CN

528116

PI 3-Kα Inhibitor VIII

The PI 3-Kα Inhibitor VIII controls the biological activity of PI 3-Kα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

PI 3-Kα Inhibitor VIII, N-((1E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-Nʹ-methyl-Nʹʹ-(2-methyl-5-nitrobenzene)sulfonohydrazide, HCl, PIK-75, PI 3-K Inhibitor VIII

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关于此项目

经验公式(希尔记法):
C16H14BrN5O4S · 2H2O · xHCl
化学文摘社编号:
分子量:
488.31 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.28
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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Quality Segment

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

pale yellow

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

[S](=O)(=O)(N(\N=C\c2[n]3c(nc2)ccc(c3)Br)C)c1c(ccc(c1)[N+](=O)[O-])C.Cl

InChI

1S/C16H14BrN5O4S.ClH/c1-11-3-5-13(22(23)24)7-15(11)27(25,26)20(2)19-9-14-8-18-16-6-4-12(17)10-21(14)16;/h3-10H,1-2H3;1H/b19-9+;

InChI key

VOUDEIAYNKZQKM-MYHMWQFYSA-N

General description

A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110α-selective PI3-K inhibitor (IC50 = 0.3, 40, 100, and 850 nM for p110α, p110γ, PI 3-K C2β, and p110β, respectively). Shown to effectively block cellular PI3-K/Akt signaling and inhibit tumor growth both in vitro (IC50 ≤58 nM in MCF7, MCF7 ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/day, i.p.).

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Kim, S., et al. 2007. Blood110, 4206.
Hayakawa, M., et al. 2007. Bioorg. Med. Chem.15, 5837.
Knight, Z.A., et al. 2007. Cell125, 733.

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)


存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable



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