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STEMCELL Technologies GDC-0941
Beskrivelse
- GDC-0941 is an inhibitor of phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)
- It inhibits class I catalytic subunits of PI3K p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively, by binding near the ATP binding pocket (Folkes et al.; Berndt et al.) It shows selectivity against class II, III, and IV PI3K isoforms as well, but with lower efficacy; for example, it inhibits phosphatidylinositol-4-phosphate 3-kinase C2 domain subunit β (C2β, Class II) and mammalian target of rapamycin (mTOR, Class IV) in the high nanomolar range and most others in the micromolar range (Folkes et al.)
- Inhibits proliferation of multiple cancer cell lines, such as U87MG (glioblastoma), PC3 (prostate) and MDA-MB-361 (breast) lines, in vitro and in mouse xenograft models (Folkes et al.; Raynaud et al.; O'Brien et al.)
- Induces apoptosis and inhibits xenograft tumor growth in combination with a MAP/ERK kinase (MEK) inhibitor GDC-0973 (Hoeflich et al.)
Tekniske data
Tekniske data
| CAS | 957054-30-7 |
| Synonym | GNE 0941; Pictilisib; Pictrelisib |
| Mængde | 10 mg |
| Molekylær formel | C23H27N7O3S2 |
| Renhed | ≥98% |
Produkttitel
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