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420104

JAK3 Inhibitor II

Name: JAK3 Inhibitor II
Brand: MM

The JAK3 Inhibitor II, also referenced under CAS 211555-04-3, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

JAK3 Inhibitor II, 4-[(3ʹ-Bromo-4ʹ-hydroxyphenyl)amino]-6,7-dimethoxyquinazoline, WHI-P154

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关于此项目

经验公式（希尔记法）:

C₁₆H₁₄BrN₃O₃

化学文摘社编号:

211555-04-3

分子量:

376.20

MDL number:

MFCD02179366

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥97% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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属性

Quality Level

100

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

pale yellow

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

Brc1c(ccc(c1)Nc2ncnc3c2cc(c(c3)OC)OC)O

InChI

1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8,21H,1-2H3,(H,18,19,20)

InChI key

CBIAKDAYHRWZCU-UHFFFAOYSA-N

说明

General description

A potent, cell-permeable, reversible, ATP-competitive, and specific inhibitor of JAK3 (IC₅₀ = 5.6 µM). Has no effect on either JAK1 or JAK2. Has also been shown to prevent the ionizing radiation-induced activation of c-Jun in DT-40 cells. Also acts as a potent inhibitor of glioblastoma cell adhesion and migration.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
JAK-3

Product competes with ATP.

Reversible: yes

Target IC₅₀: 5.6 µM against JAK3

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

Ghosh, S., et al. 2001. Acta Crystallogr. C.57, 76.
Sudbeck, E.A., et al. 1999. Clin. Cancer Res. 5, 1569.
Goodman, P.A., et al. 1998. J. Biol. Chem. 273, 17742.
Narla, R.K., et al. 1998. Clin Cancer Res.4, 2463.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

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Inhibition of human glioblastoma cell adhesion and invasion by 4-(4'-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3'-bromo-4'-hydroxylphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154).

R K Narla et al.

Clinical cancer research : an official journal of the American Association for Cancer Research, 4(10), 2463-2471 (1998-10-31)

Glioblastoma multiforme is a highly invasive primary brain tumor with a disappointingly high local recurrence rate and mortality despite intensive multimodality treatment programs. Therefore, new agents that are capable of inhibiting the infiltration of normal brain parenchyma by glioblastoma cells

4-[3-Bromo-4-hydroxyphenyl)amino]-6,7-dimethoxyquinazolin-1-ium chloride methanol solvate and 4-[(3-hydroxyphenyl)amino]-6,7-dimethoxy-1-quinazolinium chloride.

S Ghosh et al.

Acta crystallographica. Section C, Crystal structure communications, 57(Pt 1), 76-78 (2001-02-15)

The title compounds, C16H15BrN3(O3)(+).Cl(-).CH4O (WHI-P154) and C16H16N3(O3)(+).Cl(-) (WHI-P180), are potent inhibitors [WHI-P154 with IC50 = 5.6 microM and WHI-P180 with IC50 = 4.0 microM for epidermal growth factor receptor (EGFR) kinase inhibition] of the EGFR tyrosine kinase as well as

Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.

E A Sudbeck et al.

Clinical cancer research : an official journal of the American Association for Cancer Research, 5(6), 1569-1582 (1999-07-02)

A novel homology model of the kinase domain of Janus kinase (JAK) 3 was used for the structure-based design of dimethoxyquinazoline compounds with potent and specific inhibitory activity against JAK3. The active site of JAK3 in this homology model measures

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全球贸易项目编号

货号	GTIN
420104-5MG	04055977187908