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.
동의어(들):
PDGFR Tyrosine Kinase Inhibitor V, N-(4-((6,7-Dimethoxy-4-quinoyl)oxy)phenyl)-Nʹ-(2-methylbenzoyl)thiourea, Ki11502
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C26H23N3O4S · 3H2O
CAS Number:
Molecular Weight:
527.59
MDL number:
UNSPSC 코드:
12352200
추천 제품
Quality Level
분석
≥95% (HPLC)
형태
solid
제조업체/상표
Calbiochem®
저장 조건
OK to freeze
protect from light
색상
off-white
solubility
DMSO: 25 mg/mL
배송 상태
ambient
저장 온도
2-8°C
일반 설명
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.).
생화학적/생리학적 작용
Cell permeable: yes
Primary Target
PDGFR
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
포장
Packaged under inert gas
경고
Toxicity: Toxic (F)
재구성
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
기타 정보
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.
Nishioka, C., et al. 2008. Blood111, 5086.
Furuta, T., et al. 2006. J. Med. Chem.49, 2186.
법적 정보
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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
Takayuki Furuta et al.
Journal of medicinal chemistry, 49(7), 2186-2192 (2006-03-31)
We report the structure-activity relationship of quinoline and quinazoline derivatives, which include urea, thiourea, urethane, and acylthiourea groups, as inhibitors of the platelet-derived growth factor (PDGF) receptor autophosphorylation. Our previous studies showed that the quinoline and quinazoline derivatives including urea
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