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Atuveciclib

CAS No. 1414943-88-6

Atuveciclib ( BAY 1143572 | BAY1143572 )

产品货号. M11720 CAS No. 1414943-88-6

Atuveciclib (BAY-1143572) 是一种有效的、高选择性的、口服生物可利用的 CDK9/P-TEFb 抑制剂,对 CDK9/CyclinT1 的 IC50 为 6 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥2341 有现货
10MG ¥3742 有现货
25MG ¥7023 有现货
50MG ¥9396 有现货
100MG ¥12717 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Atuveciclib
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    Atuveciclib (BAY-1143572) 是一种有效的、高选择性的、口服生物可利用的 CDK9/P-TEFb 抑制剂,对 CDK9/CyclinT1 的 IC50 为 6 nM。
  • 产品描述
    Atuveciclib (BAY-1143572) is a potent, highly selective, orally bioavailable CDK9/P-TEFb inhibitor with IC50 of 6 nM for CDK9/CyclinT1; displays >150-fold selectivity over CDK1/2/3/5/6/7 (IC50>800 nM), also shows submicromolar inhibitory activity against GSK3α (IC50=45 nM), GSK3β (IC50=87?nM); demonstrates antiproliferative activity against HeLa cells (IC50=920 nM) and MOLM‐13 cells (IC50=310 nM); exhibits anticancer activity in human AML models.Blood Cancer Phase 1 Clinical.
  • 体外实验
    Atuveciclib (BAY-1143572) inhibits the proliferation of 7 MLL-rearrangements positive and negative AML cell lines with a median IC50 of 385 nM (range 230-1100 nM) and induces apoptosis. Atuveciclib (BAY-1143572) has potent and highly selective PTEFb-kinase inhibitory activity in the low nanomolar range against PTEFb/CDK9 and an at least 50-fold selectivity against other CDKs. Atuveciclib (BAY-1143572) shows a favorable selectivity against a panel of non-CDK kinases. It shows broad antiproliferative activity against a panel of tumor cell lines with sub-micromolar IC50 values. The concentration-dependent inhibition of the phosphorylation of the RNA polymerase II and downstream reduction of MYC mRNA and protein levels is observed.
  • 体内实验
    Atuveciclib (BAY-1143572) exhibits single agent efficacy at tolerated doses in 4 out of 5 AML xenograft tumor models in mice and in 2 out of 2 AML xenograft tumor models in rats upon once daily oral administration. Partial or even complete remissions could be achieved in several models.The inhibition of MYC mRNA is also observed in blood cells of Atuveciclib (BAY-1143572)-treated rats indicating the potential clinical utility of MYC in blood cells as a pharmacodynamic marker in clinical development. The in vivo efficacy of Atuveciclib (BAY-1143572) is significantly enhanced in combination with several chemotherapeutics in different solid tumor models.
  • 同义词
    BAY 1143572 | BAY1143572
  • 通路
    Cell Cycle/DNA Damage
  • 靶点
    CDK
  • 受体
    CDK
  • 研究领域
    Cancer
  • 适应症
    Blood cancer

化学信息

  • CAS Number
    1414943-88-6
  • 分子量
    387.433
  • 分子式
    C18H18FN5O2S
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO : 100 mg/mL (258.11 mM)
  • SMILES
    O=S(C)(CC1=CC=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=C1)=N
  • 化学全称
    (3-((4-(4-fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl)amino)benzyl)(imino)(methyl)-l6-sulfanone

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Lücking U, et al. ChemMedChem. 2017 Nov 8;12(21):1776-1793. 2. Narita T, et al. Blood. 2017 Aug 31;130(9):1114-1124.
产品手册
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