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Merck

521234

PDGFR Tyrosine Kinase Inhibitor V

The PDGFR Tyrosine Kinase Inhibitor V, also referenced under CAS 347155-76-4, controls the biological activity of PDGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

別名:

PDGFR Tyrosine Kinase Inhibitor V, N-(4-((6,7-Dimethoxy-4-quinoyl)oxy)phenyl)-Nʹ-(2-methylbenzoyl)thiourea, Ki11502

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この商品について

実験式(ヒル表記法):
C26H23N3O4S · 3H2O
CAS番号:
分子量:
527.59
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 25 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

S=C(Nc2ccc(cc2)Oc3c4c(ncc3)cc(c(c4)OC)OC)NC(=O)c1c(cccc1)C

InChI

1S/C26H23N3O4S/c1-16-6-4-5-7-19(16)25(30)29-26(34)28-17-8-10-18(11-9-17)33-22-12-13-27-21-15-24(32-3)23(31-2)14-20(21)22/h4-15H,1-3H3,(H2,28,29,30,34)

InChI key

ZXGIBSBJQLLUEE-UHFFFAOYSA-N

General description

A cell-permeable quinolinyl-thiourea compound that acts a potent, ATP-competitive, and reversible inhibitor of PDGFR (IC50 = 4 and 7.6 nM in ligand-induced cellular PDGFR phosphorylation and in in vitro kinase activity, respectively). Inhibits c-kit receptor only at much higher concentrations (IC50 = 434 and 234 nM in receptor phosphorylation and kinase activity, respectively). Shown to potently inhibit neointima formation in a rat carotid artery balloon injury model in vivo (30 mg/kg, p.o.).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PDGFR
Product competes with ATP.
Reversible: yes
Target IC50: 4 and 7.6 nM in ligand-induced cellular PDGFR phosphorylation and in in vitro kinase activity, respectively

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

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Getachew, R., et al. 2009. Eur. J. Pharmacol. In press.
Nishioka, C., et al. 2008. Blood111, 5086.
Furuta, T., et al. 2006. J. Med. Chem.49, 2186.

Legal Information

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

Disclaimer

Toxicity: Toxic (F)


保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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