keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
YX-2-107 是一种具有选择性和高效性的降解 CDK6 的 PROTAC ,IC50 值为 4.4 nM。YX-2-107 在体外对 RB 磷酸化和 FOXM1 表达有抑制作用,对大鼠体内 Ph+ ALL 的发展有抑制作用。YX-2-107 可用于预防和治疗 Ph 染色体阳性 (Ph+) 急性淋巴细胞白血病 (ALL)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,660 | 现货 | ||
5 mg | ¥ 4,160 | 现货 | ||
10 mg | ¥ 6,660 | 现货 | ||
25 mg | ¥ 9,880 | 现货 | ||
50 mg | ¥ 13,300 | 现货 | ||
100 mg | ¥ 17,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,570 | 现货 |
产品描述 | YX-2-107 is a selective and potent CDK6-degrading PROTAC with an IC50 value of 4.4 nM.YX-2-107 inhibits RB phosphorylation and FOXM1 expression in vitro, and inhibits the development of Ph+ ALL in rats.YX-2-107 can be used for the prophylaxis and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). YX-2-107 can be used for the prevention and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). |
靶点活性 | CDK6:4.4 nM |
体外活性 | In Ph+ BV173 and SUP-B15 cells, YX-2-107, when applied at a concentration of 2000 nM for 48 hours, demonstrates inhibition of the S phase[1]. Furthermore, at various concentrations (0, 1.6, 8, 40, 200, 1000 nM) for 4 hours, YX-2-107 selectively degrades CDK6 in BV173 cells[1]. Additionally, when used at a concentration of 2000 nM for 72 hours, YX-2-107 inhibits RB phosphorylation and FOXM1 expression in Ph+ BV173 and SUP-B15 cells[1]. |
体内活性 | Following a single intraperitoneal administration at a dose of 10 mg/kg, YX-2-107 achieves a maximum concentration of 741 nM in plasma after 4 hours. This concentration is 150-fold greater than the CDK6 degradation IC50. Clearance from the plasma is observed within the mentioned timeframe[1]. Moreover, when administered at a dose of 150 mg/kg intraperitoneally, once daily for 3 days, YX-2-107 is pharmacologically active in suppressing the proliferation of Ph+ ALL in mice[1]. |
分子量 | 889.95 |
分子式 | C45H51N11O9 |
CAS No. | 2417408-46-7 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (101.13 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.1237 mL | 5.6183 mL | 11.2366 mL | 28.0915 mL |
5 mM | 0.2247 mL | 1.1237 mL | 2.2473 mL | 5.6183 mL | |
10 mM | 0.1124 mL | 0.5618 mL | 1.1237 mL | 2.8091 mL | |
20 mM | 0.0562 mL | 0.2809 mL | 0.5618 mL | 1.4046 mL | |
50 mM | 0.0225 mL | 0.1124 mL | 0.2247 mL | 0.5618 mL | |
100 mM | 0.0112 mL | 0.0562 mL | 0.1124 mL | 0.2809 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
YX-2-107 2417408-46-7 Cell Cycle/Checkpoint CDK Inhibitor inhibitor inhibit