2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK6/9-IN-1

CDK6/9-IN-1 (compound 66) 是具有口服活性的 CDK 6 和 CDK 9 的双抑制剂，其对 CDK 6 和 CDK 9 的 IC50 值分别为 40.5 nM 和 39.5 nM。

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CDK6/9-IN-1 Chemical Structure

CDK6/9-IN-1 Chemical Structure

CAS No. : 2414373-55-8

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CDK6/9-IN-1 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively[1].

IC50 & Target[1]

CDK6

40.5 nM (IC50)

CDK9

39.5 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Jurkat IC50
4.01 μM
Compound: 66
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
[PMID: 32129996]
L02 GI50
> 100 μM
Compound: 66
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
[PMID: 32129996]
MCF7 IC50
4.01 μM
Compound: 66
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
[PMID: 32129996]
MDA-MB-231 IC50
4.01 μM
Compound: 66
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
[PMID: 32129996]
Sf9 IC50
> 10 μM
Compound: 66
Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay
Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay
[PMID: 32129996]
Sf9 IC50
0.0395 μM
Compound: 66
Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay
Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay
[PMID: 32129996]
Sf9 IC50
0.0405 μM
Compound: 66
Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay
Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay
[PMID: 32129996]
体外研究
(In Vitro)

CDK6/9-IN-1 (compound 66, 4 or 8 μM in MDA-MB-231 cells) treatment induces G0/G1 cell cycle arrest (71.85% and 77.51%, respectively), when compared with the control (57.65%)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CDK6/9-IN-1 相关抗体:
体内研究
(In Vivo)

CDK6/9-IN-1 (compound 66) significantly inhibits tumor growth in an xenograft mouse model with no obvious toxicity, indicating the promising therapeutic potential of CDK6/9 dual inhibitors for cancer treatment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

452.94

Formula

C22H25ClN8O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CDK6/9-IN-1 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK6/9-IN-12414373-55-8CDKCyclin dependent kinaseG0G1cellcyclearrestInhibitorinhibitorinhibit

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