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2070014-90-1

中文名稱 CS-1207
英文名稱 LY 303511 (hydrochloride)
CAS 2070014-90-1
分子式 C19H19ClN2O2
分子量 342.82
MOL 文件 2070014-90-1.mol
更新日期 2023/03/20 15:41:23
2070014-90-1 結(jié)構(gòu)式 2070014-90-1 結(jié)構(gòu)式

基本信息

中文別名
LY303511鹽酸鹽
化合物L(fēng)Y303511 HYDROCHLORIDE
MTOR抑制劑(LY 303511 HYDROCHLORIDE)
英文別名
CS-1207
LY 303511 (hydrochloride)

物理化學(xué)性質(zhì)

儲(chǔ)存條件Inert atmosphere,Room Temperature
形態(tài)Solid
顏色White to light yellow
CS-1207價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-15643ACS-1207
LY 303511 hydrochloride
2070014-90-15mg800元
2024/11/08HY-15643ACS-1207
LY 303511 hydrochloride
2070014-90-110mM * 1mLin DMSO880元
2024/11/08HY-15643ACS-1207
LY 303511 hydrochloride
2070014-90-110mg1300元

常見問(wèn)題列表

生物活性
LY 303511 hydrochloride 是 是 LY294002 的一種結(jié)構(gòu)類似物,但 LY303511 不抑制 PI3K。LY303511 可增強(qiáng) SHEP-1 神經(jīng)母細(xì)胞瘤細(xì)胞的TRAIL 敏感性。LY303511 可逆地阻斷 MIN6 胰島瘤細(xì)胞中的 K+ 電流 (IC50=64.6±9.1 μM)。
靶點(diǎn)

TRAIL
IC50: 64.6±9.1 μM (K + currents, in MIN6 insulinoma cells)

體外研究

LY303511 is structurally identical to LY294002 except for a substitution of -O for -NH in the morpholine ring, and does not potently inhibit PI3K. Treatment of cells with LY303511 causes an increase in calcein spread similar to levels of LY294002. The ability of LY303511 to increase gap junctional intercellular communication (GJIC) does not occur concomitant with inhibition of phosphorylation of AKT as measured by immunoblotting. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via H 2 O 2 -MAPK activation and up-regulation of death receptors. SHEP-1 cells are exposed to varying concentrations of LY303511 (LY30), TRAIL, and a combination of the two (1 h preincubation with LY303511 followed by TRAIL for 4 hours). SHEP-1 cells are responsive to TRAIL (~10%, ~15%, and ~30% reduction in the surviving fraction at 25, 50, and 100 ng/mL, respectively); however, treatment with LY303511 (12.5, 25, or 50 μM) has no effect on cell viability. However, incubation of cells with LY303511 (25 μM) for 1 hour followed by 4 hours exposure to 50 ng/mL of TRAIL has a strong synergistic effect (~40% reduction in viable cells with LY303511+TRAIL versus ~15% with TRAIL alone). LY303511 is a negative control compound with respect to PI3K activity. In MIN6 insulinoma cells, Wortmannin (100 nM) has no effect on whole-cell outward K + currents, but LY294002 and LY303511 reversibly block currents in a dose-dependent manner (IC 50 =9.0±0.7 μM and 64.6±9.1 μM, respectively). Kv2.1 and Kv1.4 are highly expressed in beta-cells, and in Kv2.1-transfected tsA201 cells, 50 μM LY294002 and 100 μM LY303511 reversibly inhibit currents by 99% and 41%, respectively. LY303511 blocks currents with an IC 50 of 64.6±9.1 μM, with a maximal inhibition of ~90% at 500 μM (n≥5 cells at each concentration).

體內(nèi)研究

Intraperitoneal administration of vehicle or LY303511 (10 mg/kg/day) is performed when tumors reach a volume of ~150 mm 3 , at which time 35 mice have developed a tumor. After 21 days, >15% of the mice require euthanasia because of excessive tumor growth, and these data are censored due to unreliable estimates of average tumor volume. The administration of LY303511, 10 mg/kg/day, is sufficient to inhibit PC-3 tumor growth in vivo.

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