| 名称 | Taletrectinib free base |
| 描述 | Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1/NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations. |
| 体外活性 | Taletrectinib free base（1-1000 nM；72小时）对Ba/F3-TPM3-NTRK1、Ba/F3-ETV6-NTRK1、-NTRK2、-NTRK3或KM12细胞的IC50约为3-20 nM。[1] Taletrectinib free base（0.001-1000 nM；2小时）在体外剂量依赖性地抑制U-118-MG细胞中ROS1的自磷酸化。[1] Taletrectinib free base在JFCR-165、JFCR-168和MGH193-1B细胞中强效抑制ROS1自磷酸化。[1] Taletrectinib free base在10 nM时部分抑制磷酸化NTRK1，在100 nM时完全抑制。Taletrectinib free base以亚纳摩尔浓度，ATP竞争性地强效抑制重组的ROS1、NTRK1和NTRK3。在1 mM ATP存在下，Taletrectinib free base在0.2 μM时几乎完全抑制了160种激酶中的ACK、ALK、DDR1和LTK，但对其他152种激酶的抑制作用不强。[1] Taletrectinib free base有效抑制对crizotinib有抗性的ROS1二级突变，包括G2032R溶剂前突变。[1] |
| 体内活性 | Taletrectinib free base (DS-6051b) (25-200 mg/kg; 口服; 每日一次, 连续18天; 携带U-118 MG细胞的Balb-c nu/nu小鼠) 表现出抗肿瘤活性。[1] Taletrectinib free base (6.25-200毫克/千克; 口服; 每日一次, 连续8天) 在携带KM12细胞的Balb-c nu/nu小鼠中抑制NTRK重新排列的癌症。[1] Taletrectinib free base (3-100 mg/kg; 口服; 每日一次, 连续4天) 在野生型(WT)及G2032R突变型的Ba/F3-carrying小鼠中显示出快速肿瘤退缩，且没有严重的体重损失。[1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (24.66 mM), Solution.
10% DMSO+90% Saline : < 10 mg/mL (24.66 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 150 mg/mL (369.94 mM), Sonication is recommended.
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| 关键字 | Taletrectinib | ROSKinase | ROS1 | ROS Kinase | IBI-344 | IBI344 | IBI 344 | DS-6051b |
| 相关产品 | L-Cystine | Mefloquine hydrochloride | Cucurbitacin B | Crizotinib | Taletrectinib | Melamine | Phosphocreatine disodium hydrate | Lorlatinib | Uniconazole | Phosphocreatine disodium | ROS kinases-IN-2 | APG-2449 |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 抗癌化合物库 | 已知活性化合物库 | ReFRAME 相关化合物库 | 激酶抑制剂库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 抗癌药物库 |
