PI 3-Kα Inhibitor VIII

Name: PI 3-Kα Inhibitor VIII
Brand: MM

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.

Sinónimos:

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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About This Item

Fórmula empírica (notación de Hill):

C₁₆H₁₄BrN₅O₄S · 2H₂O · xHCl

Número CAS:

372196-77-5

Peso molecular:

488.31 (free base basis)

MDL number:

MFCD12546130

UNSPSC Code:

12352200

NACRES:

NA.28

Nombre del producto

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.

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

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

Quality Level

100

Categorías relacionadas

Bioactive Small Molecule Inhibitors

Disclaimer

Toxicity: Regulatory Review (Z)

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.).

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.

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.

Legal Information

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

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.

Masahiko Hayakawa et al.

Bioorganic & medicinal chemistry, 15(17), 5837-5844 (2007-07-03)

We have previously reported the imidazo[1,2-a]pyridine derivative 4 as a novel p110alpha inhibitor; however, although 4 is a potent inhibitor of p110alpha enzymatic activity and tumor cell proliferation in vitro, it is unstable in solution and ineffective in vivo. To

Insulin-like growth factor-1 regulates platelet activation through PI3-Kalpha isoform.

Soochong Kim et al.

Blood, 110(13), 4206-4213 (2007-09-11)

Platelets release insulin-like growth factor-1 (IGF-1) from alpha granules upon activation. We have investigated the regulation of IGF-1 in G(i)-dependent pathways leading to Akt activation and the role of IGF-1 in platelet activation. IGF-1 alone failed to induce platelet aggregation

A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.

Zachary A Knight et al.

Cell, 125(4), 733-747 (2006-05-02)

Phosphoinositide 3-kinases (PI3-Ks) are an important emerging class of drug targets, but the unique roles of PI3-K isoforms remain poorly defined. We describe here an approach to pharmacologically interrogate the PI3-K family. A chemically diverse panel of PI3-K inhibitors was

Context dependent isoform specific PI3K inhibition confers drug resistance in hepatocellular carcinoma cells.

Kubra Narci et al.

BMC cancer, 22(1), 320-320 (2022-03-26)

Targeted therapies for Primary liver cancer (HCC) is limited to the multi-kinase inhibitors, and not fully effective due to the resistance to these agents because of the heterogeneous molecular nature of HCC developed during chronic liver disease stages and cirrhosis.

Contenido relacionado

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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