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521234

PDGFR Tyrosine Kinase Inhibitor V

Name: PDGFR Tyrosine Kinase Inhibitor V
Brand: MM

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.

别名:

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

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关于此项目

经验公式（希尔记法）:

C₂₆H₂₃N₃O₄S · 3H₂O

化学文摘社编号:

347155-76-4

分子量:

527.59

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD12032139

Assay:

≥95% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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属性

Quality Level

100

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

说明

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)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Sclerotome-derived PDGF signaling functions as a niche cue responsible for primitive erythropoiesis.

Aihua Mao et al.

Development (Cambridge, England), 150(22) (2023-10-26)

Primitive erythropoiesis serves a vital role in embryonic development, generating primitive red blood cells responsible for transportation of oxygen throughout the body. Although diverse niche factors are known to function in definitive hematopoiesis, the microenvironment contributing to primitive hematopoiesis remains

Characterisation of Ki11502 as a potent inhibitor of PDGF beta receptor-mediated proteoglycan synthesis in vascular smooth muscle cells.

Robel Getachew et al.

European journal of pharmacology, 626(2-3), 186-192 (2009-10-13)

Platelet-derived growth factor (PDGF) receptor signalling is implicated in cardiovascular diseases such as atherosclerosis and restenosis. PDGF expression levels are elevated in atherosclerotic lesions and play a key role in migration and proliferation of vascular smooth muscle cells in the

Ki11502, a novel multitargeted receptor tyrosine kinase inhibitor, induces growth arrest and apoptosis of human leukemia cells in vitro and in vivo.

Chie Nishioka et al.

Blood, 111(10), 5086-5092 (2008-03-01)

Ki11502 is a novel multitargeted receptor tyrosine kinase (RTK) inhibitor with selectivity against platelet-derived growth factor receptor alpha/beta (PDGFRalpha/beta). Ki11502 (0.1-1 nM, 2 days) profoundly caused growth arrest, G(0)/G(1) cell-cycle arrest, and apoptosis associated with down-regulation of Bcl-2 family proteins

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货号	GTIN
521234-1MG	04055977271386