| 價(jià)格 | 詢價(jià) |
| 包裝 | 1removed |
| 最小起訂量 | 1removed |
| 發(fā)貨地 | 上海 |
| 更新日期 | 2026-04-02 |
| 中文名稱:化合物 SAR-260301 | 英文名稱:SAR-260301 |
| CAS:1260612-13-2 | 品牌: TargetMol |
| 產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 純度規(guī)格: 99.74% | 產(chǎn)品類別: 抑制劑 |
| 貨號(hào): T16841 |
| 名稱 | SAR-260301 |
| 描述 | SAR-260301 is an orally available and selective inhibitor of PI3Kβ (IC50: 23 nM). |
| 體外活性 | SAR-260301 inhibits pAktS473 (a measured IC50: 0.06 μM and an estimated IC90: 2 μM), in the UACC-62 tumor cell line assay. SAR260301 inhibits PI3Kβ-dependent proliferation/viability in low serum conditions (IC50: 196 nM), in the MEF-3T3-myr-p110β mechanistic model. SAR260301 inhibits LNCaP cell proliferation in low and high serum conditions (IC50: 2.9 and 5.0 μM, respectively), after 4-day treatment, whereas it is inactive in these conditions in PC3 cells at concentrations up to 10 μM, despite target engagement). SAR260301 also leads to antitumor activities in PTEN-deficient/BRAF-mutant human melanoma cells, inhibiting cell proliferation (IC40: 6.5 and 3.3 μM for UACC-62 and WM-266.4, respectively, after 4-day treatment). After prolonged treatment, SAR260301 at 3 or 10 μM inhibits PC3 cell proliferation in low serum conditions, with a cytostatic effect achieved for 14 days, despite some cell death induction observed at 10 μM [2]. |
| 體內(nèi)活性 | SAR-260301 is well tolerated at the active dose, with no sign of toxicity and no bodyweight loss. SAR-260301 displays antitumor efficacy in human PTEN-deficient melanoma models in mice as a single agent. SAR-260301 treatment leads to a statistically significant tumor growth inhibition as measured by a ΔT/ΔC of 39% (p = 0.054 versus control mice) on day 15 post-tumor implantation. SAR-260301(p.o.) reveals sustained target inhibition (≥50%) of pAkt-S473 for at least 7 h. SAR-260301 has moderate terminal elimination half-life (t1/2=0.87 h, 1.4 h, 2.5 h, 0.87h, 6.9 h and 4.5 h for female SCID mice (3 mg/kg, iv), mice (10 mg/kg, p.o.), mice (100 mg/kg, p.o.), female nude rats (3 mg/kg, iv), rat (10 mg/kg, p.o.), male beagle dogs (10 mg/kg, p.o.)) [1]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (11.29 mM), Sonication is recommended. DMSO : 125 mg/mL (352.71 mM), Sonication is recommended. |
| 關(guān)鍵字 | Vps34 | SAR-260301 | SAR260301 | SAR 260301 | PI3Kδ | PI3Kγ | PI3Kβ | PI3Kα | PI3KC2γ | pAkt | DNA-PK |
| 相關(guān)產(chǎn)品 | 4-Methylbenzylidene camphor | Berberine hydrogen sulphate | Creatine monohydrate | Musk ketone | Quercetin | Hyaluronic acid | Berberine sulfate | Methyl eugenol | Myricetin | Quercitrin hydrate | Isoprenaline hydrochloride | 4-Vinylcyclohexene Dioxide |
| 相關(guān)庫(kù) | 抗癌化合物庫(kù) | ReFRAME 相關(guān)化合物庫(kù) | PI3K/Akt/mTOR 化合物庫(kù) |
| 成立日期 | 2013-04-18 (14年) | 注冊(cè)資本 | 566.265100萬人民幣 |
| 員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
| 主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
| 產(chǎn)品名稱 | 價(jià)格 | 公司名稱 | 報(bào)價(jià)日期 | |
|---|---|---|---|---|
| ¥1000 |
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