2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. DNA-PK
  4. DNA-PK-IN-8

DNA-PK-IN-8 (compound DK1) 是一种高效且具有选择性和口服活性的 DNA 依赖蛋白激酶 (DNA-PK) 抑制剂，IC50 为 0.8 nM。DNA-PK-IN-8 与 Doxorubicin 联合使用时，对一系列癌细胞具有协同抗增殖活性，并能显著抑制 HL-60 肿瘤的生长。

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DNA-PK-IN-8 Chemical Structure

DNA-PK-IN-8 Chemical Structure

CAS No. : 2823369-81-7

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DNA-PK-IN-8 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin[1].

IC50 & Target

IC50: 0.8 nM (DNA-PK)[1]
体外研究
(In Vitro)

DNA-PK-IN-8 (compound DK1) decreases the expression levels of γH2A.X in a concentration-dependent manner in HCT-116 cells[1].

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

DNA-PK-IN-8 相关抗体:

Immunofluorescence

Cell Line: HCT-116 (treated with Bleomycin for 6 hours)[1]
Concentration: 1, 5, and 10 μM
Incubation Time: 6 hours
Result: Decreased the expression levels of γH2A.X in a concentration-dependent manner.
体内研究
(In Vivo)

DNA-PK-IN-8 (100 mg/kg; PO; QD for 16 days) significantly suppresses HL-60 tumor growth when co-administrating with Doxorubicin[1].
DNA-PK-IN-8 (5 mg/kg; PO; single dosage) exhibits reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate[1].
Pharmacokinetic Parameters of DNA-PK-IN-8 in Sprague-Dawley rats[1].

PO (5 mg/kg)
Tmax (h) 0.42 ± 0.11
t1/2 (h) 1.59 ± 0.26
Cmax (ng/mL) 810 ± 122.32
AUC0-∞ (ng/mL·h) 3598.7 ± 769.81
MRT0-∞ (h) 2.29 ± 0.18

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

Animal Model: HL-60 tumor-bearing nude mice model[1]
Dosage: 100 mg/kg
Administration: PO; QD for 16 days
Result: Led to significant tumor-suppressing effects with TGI values of 52.4% and 62.4% for tumor weight and tumor volume, respectively, when co-administrated with Doxorubicin.
Animal Model: Sprague-Dawley rats[1]
Dosage: 5 mg/kg
Administration: PO; single dosage (Pharmacokinetic Analysis)
Result: Exhibited reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate.
分子量

394.43

Formula

C19H22N8O2
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

DNA-PK-IN-8 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:

DNA-PK-IN-82823369-81-7DNA-PKDNA-dependent protein kinaseAnticancerDNADamage responseDSBHCT-116HL-60AntiproliferativeInhibitorinhibitorinhibit

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