| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408320-1ml |
1ml |
现货  |
|
| 英文别名 | RG7422, GNE 390 | (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Apitolisib (GDC-0980) |
| 生化机理 | Apitolisib （GDC-0980、RG7422、GNE 390）是一种强效的 I 类 PI3K 抑制剂，在无细胞实验中对 PI3Kα/β/δ/γ 的 IC50 分别为 5 nM/27 nM/7 nM/14 nM。它也是一种 mTOR 抑制剂，在无细胞实验中的Ki值为 17 nM，对其他 PIKK 家族激酶具有高度选择性。Apitolisib 可同时激活胰腺癌细胞的自噬和凋亡。第二阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | PI3 激酶 I 类抑制剂 |
| 产品介绍 |
Apitolisib (GDC-0980, RG7422, GNE 390)是一种有效的，I型PI3K抑制剂，作用于PI3Kα/β/δ/γ，无细胞试验中IC50分别为5 nM/27 nM/7 nM/14 nM，也是mTOR抑制剂，无细胞试验中Ki为17 nM，比作用于其他PIKK家族激酶选择性高。Apitolisib 在胰腺癌细胞中可同时激活自噬与凋亡。 Information Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor forPI3Kα/β/δ/γwithIC50of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also amTORinhibitor withKiof 17 nM in a cell-free assay, and highly selective versus other PIKK fa GDC-0980 shows the potent and selective inhibitory activities against class I PI3K and mTOR kinase versus a large panel of kinases with Ki of 17 nM for mTOR and IC50 of 5 nM, 27 nM, 7 nM, and 14 nM for PI3Kα, β, δ, and γ, respectively. In vitro, GDC-0980 significantly inhibits cell proliferation in PC3 and MCF7 cells with IC50 of 307 nM and 255 nM, respectively. A recent study shows that GDC-0980 reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nM 100%), breast (IC50 <200 nM 37%, <500 nM 78%) and NSCLC lines (IC50 <200 nM 29%, <500 nM 88%) and less potency in pancreatic (IC50 <200 nM 13%, <500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%, <500 nM 33%). In vivo In both PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg, exhibits significant antitumor activity by causing tumor growth delay. Furthermore, GDC-0980 results in tumor stasis or regressions at the maximum tolerated dose of 7.5 mg/kg. In mice, intravenous GDC-0980 administration at 1 mg/kg leads to low clearance (Clp: 9.2 mL/min/kg, Vss: 1.7 L/kg). While, oral administration at 5 mg/kg in 80% PEG400 and at 50 mg/kg as a crystalline suspension in 0.5% methylcellulose/0.2% Tween-80 also results in favorable pharmacokinetic parameters. cell lines： Concentrations：0 to 10 μM Incubation Time：72 hours or 96 hours Powder Purity:≥97% |
| ALogP | 0.2 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)C(=O)[C@H](C)O |
| 分子量 | 498.61 |
| Reaxy-Rn | 29348927 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29348927&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 92 mg/mL (199.78 mM); Ethanol: 3 mg/mL (6.51 mM); Water: Insoluble; |
|---|---|
| 折光率 | 1.68 |
| 沸点 | ~718.6° C at 760 mmHg |
| 熔点 | 222-226°C |
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