Name: Lerociclib
Brand: TargetMol
SKU: T11345
Price: 412 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 412

现货

5 mg

¥ 993

现货

10 mg

¥ 1,590

现货

25 mg

¥ 2,830

现货

50 mg

¥ 4,130

现货

100 mg

¥ 5,880

现货

200 mg

¥ 8,150

现货

生物活性

产品描述	Lerociclib (G1T38) is a selective and highly potent CDK4/6 inhibitor with anticancer and antitumor activity, inhibits CDK4/CyclinD1 and CDK6/CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended.
靶点活性	CDK9-CyclinT:28 nM, CDK5-p25:1.2 μM, CDK5-p35:0.832 μM, CDK1-cyclinB1:2.4 μM, CDK2-CyclinE:3.6 μM, CDK4/6 dependent cells:20 nmol/L (EC50), CDK7-CyclinH-MAT1:2.4 μM, Cdk4-CyclinD1:1 nM, CDK2-CyclinA:1.5 μM, CDK6-CyclinD3:2 nM
体外活性	与 CDK1、CDK2、CDK5 和 CDK7 及其各自的结合伙伴相比，Lerociclib 对 CDK4/cyclin D1 和 CDK6/cyclin D3 具有很高的效力和选择性。Lerociclib 能在依赖 CDK4/6 的细胞中产生强效、持续的 G1 停滞，EC50 约为 20 nmol/L。[1]
体内活性	为了评估 Lerociclib 在小鼠中的 PK/PD 关系，采用了一种 ER+ MCF7 异种移植模型。对单次口服 Lerociclib （100 毫克/千克）的肿瘤小鼠血浆和肿瘤中的化合物浓度进行了测定。口服 Lerociclib 有足够的小鼠 PK/PD，可用于评估肿瘤模型的疗效。[1]
别名	G1T-38, G1T38, G1T 38

化学信息

分子量	474.6
分子式	C₂₆H₃₄N₈O
CAS No.	1628256-23-4
Smiles	O=C1NCC2(N3C=4N=C(N=CC4C=C13)NC5=NC=C(C=C5)N6CCN(CC6)C(C)C)CCCCC2
密度	1.41 g/cm3 (Predicted)

储存&溶解度

存储	store at low temperature,keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.