2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Membrane Transporter/Ion Channel
  3. DNA-PK BCRP
  4. Nedisertib

Nedisertib  (Synonyms: Peposertib; M3814)

目录号: HY-101570G
产品使用指南 技术支持

Nedisertib (GMP) (Peposertib (GMP)) 是 GMP 级别的 Nedisertib (HY-101570)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。Nedisertib (Peposertib) 是一种口服有效的选择性 DNA 依赖性蛋白激酶 (DNA-PK) 抑制剂，IC50 值小于 3 nM。Nedisertib 也是 ABCG2 的调节剂，可逆转 ABCG2 介导的多药耐药 (MDR)，为联合用药提供新策略。Nedisertib 可通过抑制 DNA 双链断裂修复增强化疗或放疗效果。Nedisertib 具有抗肿瘤的活性。

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Nedisertib

Nedisertib Chemical Structure

CAS No. : 1637542-33-6

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Nedisertib 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

Nedisertib (GMP) (Peposertib (GMP)) is Nedisertib (HY-101570) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Nedisertib is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity[1][2][3].

体外研究
(In Vitro)

Nedisertib (GMP) (0.3-1 µM; 72 h) 在 ABCG2 过表达的肺癌细胞系 NCI-H460/MX20 和 A549/MX10 中可显著增强 ABCG2 底物药物Mitoxantrone (HY-13502) 和 Doxorubicin (HY-15142A) 的细胞毒性，逆转多药耐药[1]。

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

Nedisertib 相关抗体:
体内研究
(In Vivo)

Nedisertib (GMP) (25-300 mg/kg; 口服; 单剂量) 在多种异种移植肿瘤模型中，增强了电离辐射的抗肿瘤效果[2]。

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

Animal Model: 6 human xenograft models (HCT116, FaDu, NCI-H460, A549, Capan-1, BxPC3) in mice representing 4 different cancer types (colon, head and neck, lung, and pancreas) treated ionizing radiation (IR)[2]
Dosage: 25-300 mg/kg
Administration: Oral administration; single dose; 10 min prior to IR
Result: Significantly inhibited tumor growth in all 6 models in combination with IR.
Induced tumor regression in FaDu and NCI-H460 models, and showed no tumor regrowth in the FaDu model with the combination of 25 and 50 mg/kg and IR (total 60 Gy).
Had no significant weight loss or visual signs of toxicity in mice.
分子量

481.91

Formula

C24H21ClFN5O3
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

Nedisertib 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

Nedisertib (GMP)1637542-33-6Peposertib (GMP)M3814 (GMP)DNA-PKBCRPDNA-dependent protein kinaseBreast cancer resistance proteinABCG2Inhibitorinhibitorinhibit

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