货号	规格	价格	上海	北京	珠海	重庆	武汉
S89134-1mg买3赠1	99.40%	￥210.00 S89134-1mg ￥210.00 现货（买3赠1）	8 8	-	-	-	-
S89134-5mg买3赠1	99.40%	￥620.00 S89134-5mg ￥620.00 现货（买3赠1）	5 5	-	-	-	-
S89134-10mg买3赠1	99.40%	￥1060.00 S89134-10mg ￥1060.00 现货（买3赠1）	5 5	-	-	-	-
S89134-25mg买3赠1	99.40%	￥2130.00 S89134-25mg ￥2130.00 现货（买3赠1）	5 5	-	-	-	-
S89134-100mg	≥98%	￥5280.00 S89134-100mg ￥5280.00 2-3天	0 货期：2-3天	-	-	-	-

大包装询价收藏产品

加入购物车

产品描述：

CDKI-73 (LS-007) 是一种有效的 CDK 抑制剂，对CDK1、CDK2、CDK4和CDK9的IC50值分别为8.17 nM，3.27 nM，8.18 nM和5.78 nM。CDKI-73 可诱导癌细胞的凋亡。CDKI-73 是一种口服生物利用型且高效的 CDK9 抑制剂，可用于治疗急性髓细胞性白血病

靶点：

CDK2(Cell-free assay):3.27 nM; CDK9(Cell-free assay):5.78 nM; CDK1(Cell-free assay):8.17 nM; CDK4(Cell-free assay):8.18 nM;Apoptosis; CDK

体外研究：

CDKI-73 induces cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. Contrastively, it is relatively low toxic to the bone marrow cells of healthy donors

体内研究：

CDKI-73 is orally bioavailable, highly efficacious against MLL-AML MV4–11 xenografts and downregulates anti-apoptotic proteins by targeting CDK9 in vivo

细胞实验：

Cell lines: Leukemia cell lines (MOLM13, MV4-11, THP-1, etc.) Concentrations: 0.05 μM, 0.1 μM, 0.25 μM, 0.5 μM Incubation Time: 1 h, 4 h, 12 h, 24 h, 48 h Method: MV4-11 (1 × 105/well) cells are seeded and incubated under 5% CO2 at 37ºC overnight. After incubation with indicated concentrations of the CDKI-73 for 24 or 48 h, cells are collected and centrifuged (300 g, 5 min). For cell cycle assay, the pellets are re-suspended in cold 70% ethanol and fixed on ice for 15 min, followed by centrifugation (300 g, 5 min). The collected pellets are incubated with 200 μL staining solution at 37ºC for 1 h, then analyzed with a Gallios flow cytometer. Apoptosis is assessed with cells collected and processed as per the instruction in the annexin V-FITC/PI commercial kit

动物实验：

Animal Models: female nude (nu/nu) Balb/C mice aged 6–8 weeks Dosages: 25 mg/kg Administration: Oral gavage

参考文献：

1. Shao Xie, et al. Antitumor action of CDK inhibitor LS-007 as a single agent and in combination with ABT-199 against human acute leukemia cells. Acta Pharmacol Sin. 2016 Nov;37(11):1481-1489. 2. Muhammed H Rahaman, et al. CDKI-73: an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia. Invest New Drugs. 2019 Aug;37(4):625-635.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.535 ml	12.676 ml	25.352 ml
5 mM	0.507 ml	2.535 ml	5.07 ml
10 mM	0.254 ml	1.268 ml	2.535 ml
50 mM	0.051 ml	0.254 ml	0.507 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置