1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  2. Phosphodiesterase (PDE) DNA/RNA Synthesis Apoptosis Ferroptosis
  3. TDP1-IN-6

TDP1-IN-6 (Compound 16b) 是一种 TDP1 抑制剂,其 IC50 为 1.52 μM。TDP1-IN-6 联合 Topotecan (HY-13768) 可增强 DNA 损伤、诱导凋亡 (Apoptosis)、诱导 S 期细胞周期阻滞、诱导铁死亡 (Ferroptosis)。TDP1-IN-6 可用于宫颈癌的研究。

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TDP1-IN-6

TDP1-IN-6 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TDP1-IN-6 (Compound 16b) is a TDP1 inhibitor with an IC50 of 1.52 μM. Combination of TDP1-IN-6 with Topotecan (HY-13768) enhances DNA damage, induces Apoptosis, triggers S-phase cell cycle arrest, and promotes Ferroptosis. TDP1-IN-6 can be used for the research of cervical cancer[1].

体外研究
(In Vitro)

TDP1-IN-6 可通过稳定结合蛋白的催化结构域和 DNA 结合结构域,强效抑制纯化的 TDP1 酶,其 IC50 为 1.52 μM[1]
TDP1-IN-6 可抑制 HeLa 宫颈癌细胞活力,其 IC50 为 14.85 μM;与 Topotecan 联用时可产生协同细胞毒性作用[1]
TDP1-IN-6 (2-4 μM combined with 2 μM TPT) 可通过调控凋亡相关蛋白 (包括下调 BCL-2、上调 BAX 和活化的胱天蛋白酶),以剂量依赖的方式增强 Topotecan 诱导的 HeLa 宫颈癌细胞凋亡[1]

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

Cell Proliferation Assay[1]

Cell Line: HeLa cervical cancer cells
Concentration: 2-4 μM TDP1-IN-6; 2 μM TPT
Incubation Time: 72 h (wound healing)
Result: Had no effect on colony formation, wound healing, or cell invasion when used alone.
Significantly reduced colony formation rates when combined with TPT: 0.50 for 2 μM TPT + 2 μM TDP1-IN-6; 0.33 for 2 μM TPT + 4 μM TDP1-IN-6.
Slowed wound healing when combined with TPT: 0.46 and 0.28 wound healing rates at 72 h for 2 μM TPT + 2 μM TDP1-IN-6 and 2 μM TPT + 4 μM TDP1-IN-6, respectively.
Reduced invasive cell counts by ~81.5% for 2 μM TPT + 4 μM TDP1-IN-6 compared to control when combined with TPT.
药代动力学
(Parmacokinetics)
Species Dose Route Bioavailability
Mice[1] 5 mg/kg i.p. 62.7 %
Mice[1] 10 mg/kg i.p. 71.6 %
体内研究
(In Vivo)

TDP1-IN-6 (5-10 mg/kg;腹腔注射;每 2 天 1 次) 单独使用在 HeLa 宫颈癌异种移植模型中未表现出显著的抗肿瘤活性,但与 Topotecan 联用时,可发挥强效的协同肿瘤生长抑制作用,且仅产生极低的额外毒性[1]

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

Animal Model: Female nude mice (SPF grade)[1]
Dosage: 5 mg/kg (monotherapy; combination with TPT); 10 mg/kg (monotherapy; combination with TPT); 0.3 mg/kg (TPT, combination)
Administration: i.p.; every 2 days
Result: Did not significantly reduce tumor growth compared to control group (monotherapy at 5 mg/kg or 10 mg/kg).
Significantly inhibited tumor growth when combined with 0.3 mg/kg TPT, resulting in significantly lower tumor weights at study end point (5 mg/kg and 10 mg/kg).
Caused only slight decreases in mouse body weight (monotherapy).
Did not exacerbate body weight loss when coadministered with TPT.
Showed extensive necrotic areas and inflammatory cell infiltration in tumors from combination treatment groups.
分子量

522.60

Formula

C29H30N8O2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
TDP1-IN-6
目录号:
HY-183546
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