Pyrimidines And Derivatives

Medchemexpress LLC Methanone, (4-amino-1,3-dihydrofuro[3,4-c]naphthyridin-8-yl)[(3S)-3-[4-(trifluoromethyl)phenyl]-4-morpholiny | 2790567-82-5 | C22H19F3N4O3 | 250 MG

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AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. When complexed with MTA, it preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5, while protecting normal cells with wild-type MTAP. This compound is for research use only.

• Preferentially inhibits the growth of MTAP-deficient tumor cells
• Inhibits PRMT5 with an IC50 of 0.107 μM
• Protects normal cells with wild-type MTAP
• Induces alternative splicing defects, cell cycle arrest, and DNA damage response in MTAP-deficient HCT116 cells
• Reduces S phase and increases G2/M cell population in MTAP-deficient cells
• Dose-dependently inhibits tumor growth in MTAP-deficient xenograft mice
• Causes tumor regression in 70% of mice with DLBCL tumors
• Preserves normal hematopoietic cell lineages

Medchemexpress LLC HY-10115 100mg Medchemexpress, PI-103 CAS:371935-74-9 Purity:98%

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Medchemexpress,HY-10115 100mg PI-103 CAS:371935-74-9 Formula:C19H16N4O3 PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. Purity:98% Medchemexpress has over 10000 novel life-science reagents, reference compounds, APIs and natural compounds for laboratory and scientific use. Other quantity can also be offered.

Medchemexpress LLC PKI-179 hydrochloride | 1463510-35-1 | 99.66% | 525.00 | 500 UG

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PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor. It shows IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ, and mTOR, respectively. It also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride has demonstrated anti-tumor activity in vivo.

• Potent and orally active dual PI3K/mTOR inhibitor.
• Exhibits activity against various PI3K isoforms (PI3K-α, PI3K-β, PI3K-γ, PI3K-δ) and mTOR.
• Active against E545K and H1047R.
• Shows anti-tumor activity in vivo.
• Inhibits cell proliferation in MDA361 and PC3 cells.
• Good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min).