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Chemdea |
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TG100-115 -
PI3Kγ/δ Inhibitor |
Catalog # CD0287 |
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Price: 1 mg - $75;
5 mg - $95; 10 mg - $150; 25 mg - $250; 50 mg - $450; 100 mg - $850; 200 mg -
$1500; 500 mg - $2500; 1 g - $4500 |
Availability: In stock |
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3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol
(6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine)
Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 98% by HPLC. CAS# 677297-51-7. Solubility: DMSO (1 mg/mL). Molecular Formula: C18H14N6O2. Molecular Weight: 346.34.
TG100-115 inhibited PI3Kγ and PI3Kδ (IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and PI3Kβ were relatively unaffected (IC50 values >1 μM). In 133 protein kinase panel, TG100-115 did not show significant inhibition (IC50 values >1 μM). In a mouse murine asthma model, TG100-115 markedly reduced the pulmonary eosinophilia and the concomitant interleukin-13 and mucin accumulation. TG100-115 also inhibited inflammatory patterns in mouse smoke model. In a rat and porcine model of myocardial infraction TG100-115 potently inhibited edema and inflammation in response to multiple mediators, including vascular endothelial growth factor and platelet-activating factor. By contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage, was not disrupted. References: 1. Doukas, J., et al. J. Pharmacol. Exp. Ther. 2009, 328, 758; 2. Doukas, J., et al. Biochem. Soc. Trans. 2007, 35, 204; 3. Doukas, J., et al. Proc. Natl. Acad. Sci. U.S.A. 2006, 103, 19866. |
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CHEMDEA; |