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Product introduction

Ribociclib (LEE011) 是一种高度特异性的CDK4和CDK6抑制剂，对应的IC50值分别为10 nM和39 nM。Phase 3。 LEE011（NVP-LEE011）是高度特异性的CDK4/CDK6抑制剂，通过减少磷酸化的RB和FOXM1来发挥作用。在17种人神经母细胞瘤细胞系中， 12种对LEE011敏感，平均IC50值为306±68 nM。 CDK4/6可通过磷酸化肿瘤抑制蛋白RB来增加G1-S期细胞周期的进程，从而诱导细胞增殖。CDK4/6信号也可以通过调节FOXM1转录来抑制衰老[3]。大量研究表明，CDK4/CDK6的过表达与肿瘤发生和疾病进展相关。 LEE011是一种新型的CDK4/CDK6抑制剂。在人脂肪肉瘤细胞系中，LEE011可通过阻滞G0-G1细胞周期，显著抑制细胞生长。在12/17种人神经母细胞瘤来源的细胞系中，LEE011处理后可显著减少细胞增殖。在异种移植人脂肪肉瘤的小鼠模型中，LEE011持续口服治疗后可以抑制肿瘤生长或诱导肿瘤衰退，而对小鼠的体重没有产生不利影响。在异种移植神经母细胞瘤细胞的小鼠中，LEE011治疗可抑制肿瘤生长。

Specs ⸢ View details ⸥

Chinese name

瑞博西利, 细胞周期蛋白依赖性激酶 6 抑制剂

English name

Ribociclib

Chinese alias

瑞博西林

English alias

Cambridge id 5121815 | DB11730 | Q27088552 | AC-30029 | Ribociclib [INN] | 6ZZ | BCP08804 | SW220101-1 | FT-0700117 | TK8ERE8P56 | HY-15777 | 7-Cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide | B

CAS number

1211441-98-3

molecular formula

C23H30N8O

molecular weight

434.5 g/mol

Exact mass

PSA

91.200 Å²

Logp

2.2

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LEE011 Rui Bo Si Ke Li Bu 10mM in DMSO 1ml

Name: LEE011 Rui Bo Si Ke Li Bu 10mM in DMSO 1ml
Brand: 麦克林
SKU: R795894-1ml

LEE011 Rui Bo Si Ke Li Bu 10mM in DMSO 1ml Macklin 1211441-98-3, complete specifications, for production, research, laboratory testing and inspection, digital one-stop procurement platform for scientific materials.

item number：R795894-1ml

Product model：1ml

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Lead Time：30days

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LEE011 Rui Bo Si Ke Li Bu 10mM in DMSO 1ml

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