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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1276553-09-3
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥670.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥354.0 |
| 规格： | 5 mg | 产品价格： | ￥800.0 |
| 规格： | 10 mg | 产品价格： | ￥1280.0 |
| 规格： | 25 mg | 产品价格： | ￥2488.0 |
| 规格： | 50 mg | 产品价格： | ￥3900.0 |
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PF-4989216
CAS No. : 1276553-09-3
MCE 国际站：PF-4989216
产品活性：PF-4989216 是一种有效的选择性 PI3Kα 抑制剂，Ki 为 0.6 nM。
研究领域：PI3K/Akt/mTOR | Apoptosis
In Vitro: PF-4989216 (Compound 10) has excellent PI3Kα Ki (0.6 nM), good cellular potency (S473 IC50=79 nM), and good selectivity against mTOR (mTOR Ki=1440 nM). PF-4989216 has PI3Kα Ki less than 1 nM and mTOR Ki more than 1 μM. PF-4989216 also has excellent selectivity over 40 other kinases, and no major CYP inhibitions are observed. Less than 30% inhibition is observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM. The toxicity of PF-4989216 in several drug-sensitive and MDR cancer cell lines, including cells overexpressing ABCB1 or ABCG2, and in HEK293 cells transfected with human ABCB1 or ABCG2 is determined. PF-4989216 inhibits human colon carcinoma S1 cell line and ABCG2-overexpressing subline S1-M1-80 with IC50s of 1.11±0.09 and 6.79±1.00 uM, respectively. PF-4989216 inhibits human breast carcinoma MCF-7 and ABCG2-overexpressing sublines MCF7-FLV1000 and MCF7-AdVp3000 IC50s of 2.30±0.68, 23.26±2.94 and 62.57±5.46 uM, respectively. PF-4989216 inhibits pcDNA-HEK293, ABCB1-transected MDR19-HEK293, ABCG2-tranfected R482-HEK293 cells with IC50s of 0.44±0.05, 0.38±0.06 and 5.05±0.89 uM, respectively.
In Vivo: PF-4989216 (Compound 10) is dosed orally in our in vivo antitumor model, PI3K driven NCI-H1975 xenograft tumors. PF-4989216 demonstrates dose responsive tumor growth inhibitory activity from 25 to 200 mg/kg in QD oral dosing.
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文献和实验,L.D. TITLE Utilization of transcription factor Brn-3a JOURNAL Patent: JP 2001511344-A 2 14-AUG-2001; NEUROVEX LTD COMMENT OS Mus musculus (mouse) PN JP 2001511344-A/2 PD 14-AUG-2001 PF 27-JUL-1998 JP 2000504246 PR 25-JUL-1997 GB 9715823.2,10
光明亮；3+～4+为荧光闪亮。 73.碱性磷酸酶-抗碱性磷酸酶桥联酶标法检测 阳性细胞等于或大于20%为阳性结果 74.末端脱氧核苷酰转移酶（TdT）检测（同位素检测法） 正常人骨髓细胞的活性为dGTP掺入1×108个细胞的量为0～0.09mmol/L 75.末端脱氧核苷酰转移酶（TdT）检测（酶标免疫细胞化学显示法） 阳性反应为棕黄色颗粒，定位在细胞核上。TdT为早期T淋巴细胞的标志，在正常情况下不成熟的胸腺淋巴细胞出现阳性反应，正常
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