2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK9-IN-19

CDK9-IN-19 是高效且具有选择性的 CDK9 抑制剂，IC50 为 2.0 nM。CDK9-IN-19 具有良好的癌细胞抗增殖活性、中等药代动力学特性和较低的 hERG 抑制活性。CDK9-IN-19 在 MV4-11 异种移植小鼠模型中显著抑制肿瘤生长。CDK9-IN-19可用于研究急性髓系白血病 (AML) 。

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CDK9-IN-19 Chemical Structure

CDK9-IN-19 Chemical Structure

CAS No. : 2479306-60-8

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CDK9-IN-19 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

CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML)[1].

IC50 & Target[1]

CDK9/cyclinT1

2 nM (IC50)

体外研究
(In Vitro)

CDK9-IN-19 (compound 30i) has antiproliferative activity against a panel of human tumor cell lines with IC50 ranks of 0.08~0.64 μM (for example: Hep G2, HCT-116, SW620, A549, MV-4-11, et al.)[1].
CDK9-IN-19 has low hERG inhibitory activity (IC50=10080 nM) and over 5000-fold selectivity for CDK9[1].
CDK9-IN-19 (0.1-0.8 μM; 24 h) reduces the expression levels of Mcl-1 and c-Myc[1].

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

CDK9-IN-19 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.2, 0.4 and 0.8 μM
Incubation Time: 24 h
Result: Clearly reduced the expression levels of Mcl-1 and c-Myc at 0.1 μM, and completely reduced at 0.2-0.8 μM.
体内研究
(In Vivo)

CDK9-IN-19 (10, 20 or 40 mg/kg; IV, for 32 days) significantly suppresses the tumour progression in MV4-11 xenograft model[1].
Pharmacokinetic Parameters of CDK9-IN-19 in ICR mice[1].

PO (30 mg/kg) IV (2 mg/kg)
T1/2 (h) NR 0.23
Tmax (h) 0.25 -
C0 (ng/mL) - 3060
Cmax (ng/mL) 665 -
AUC0-t (ng/mL·h) 1200 560
AUC0-∞ (ng/mL·h) NR 561
CL (L/h/kg) - 3.56
VdSS (L/kg) - 0.67
F (%) 14.3 -

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

Animal Model: Female BALB/c nude mice (injected with MV4-11)[1]
Dosage: 10, 20 or 40 mg/kg
Administration: IV, for 32 days
Result: Significantly suppressed the tumour progression and tumour growth inhibition (TGI) values up to 100% from days 14-32 at 40 mg/kg.
分子量

508.47

Formula

C26H22F2N4O5
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

CDK9-IN-19 相关分类

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  • 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:

CDK9-IN-192479306-60-8CDKCyclin dependent kinaseanticancerantiproliferativeantitumorMV4-11AMLCDK9BALB/c micexenograftInhibitorinhibitorinhibit

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