GNE-9605
| CAS | 1536200-31-3 |
| 分子式 | C17H20ClF4N7O |
| 分子量 | 449.83 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| SMILES | FC(C1=CN=C(NC2=C(Cl)N([C@@H]3[C@@H](F)CN(C4COC4)CC3)N=C2)N=C1NC)(F)F |
| 靶点 | LRRK2 |
| 规格 | 5mg 10mg |
GNE-272CAS号： 1936428-93-1分子式： C22H25FN6O2分子量： 424.2描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
GNE-272 is a in Vivo Probe for the Bromodomains of CBP/EP300. |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
GNE272,GNE 272
|
| 外观 |
Powder
|
| 可溶性/溶解性 |
DMSO : ≥ 150 mg/mL (353.38 mM)
|
| 生物活性 | |
| 靶点 |
Histone Acetyltransferase
|
| In vitro(体外研究) |
GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4−11 cell line) with an EC50 of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed.
|
| In vivo(体内研究) |
GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model.
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分子结构图
GNE-0877
| 别名 | GNE0877 |
| CAS | 1374828-69-9 |
| 分子式 | C14H16F3N7 |
| 分子量 | 339.32 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| SMILES | CC1=NN(C(C)(C)C#N)C=C1NC2=NC=C(C(F)(F)F)C(NC)=N2 |
| 靶点 | LRRK2 |
| 规格 | 5mg 10mg |
GNE-7915
| 别名 | gne7915 |
| CAS | 1351761-44-8 |
| 分子式 | C19H21F4N5O3 |
| 分子量 | 443.4 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | GNE-7915是高效选择性，可渗透大脑的LRRK2抑制剂，IC50值为9 nM。[1-2] |
| In Vitro | 维持C-2’/ C-5’的甲氧基/氟代排列和不同的氨基烷基R1取代导致GNE-7915和化合物19的单位数纳摩尔LRRK2细胞活性。扩增的Invitrogen激酶分析（187种激酶），0.1μM GNE-7915（比LRRK2 Ki高100倍）和19（比LRRK2 Ki高250倍）仅在TTK中产生显示大于50％的抑制。使用DiscoverX KinomeScan55竞争性结合测定组（包括392种独特激酶）的选择性分析也以0.1μM对GNE-7915进行。对于10种激酶检测> 50％探针置换的结合，对于仅LRRK2，TTK和ALK检测> 65％的结合，进一步支持对GNE-7915的优异LRRK2选择性。 Cerep受体分析，包括扩大的脑组，提示GNE-7915和19仅抑制5-HT2B，在10μM时抑制> 70％。 GNE-7915和19被证实是中等强效的5-HT2B拮抗剂体外功能测定[2]。 |
| SMILES | CCNC1=NC(NC2=C(OC)C=C(C(N3CCOCC3)=O)C(F)=C2)=NC=C1C(F)(F)F |
| 靶点 | LRRK2 |
| 数据来源文献 | [1]. Kavanagh ME, et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3690-6.
[2]. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2012 Nov 26;55(22):9416-33 |
| 规格 | 5mg 10mg 25mg |
是高效选择性的LRRK2抑制剂。