2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Epigenetics Apoptosis
  3. HSP Aurora Kinase Apoptosis
  4. NN-01-195

NN-01-195 是一种 HSP90 抑制剂药物偶联物。NN-01-195 能紧密结合并抑制 AURKA 和 HSP90，对 AURKA 的 IC50 为 3.1 nM，对 HSP90α 的 IC50 为 8.7 nM。NN-01-195 在肿瘤细胞中可导致有丝分裂停滞和纺锤体异常，诱导细胞凋亡 (apoptosis)。NN-01-195 可用于实体瘤的研究。

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NN-01-195

NN-01-195 Chemical Structure

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NN-01-195 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

查看 Aurora Kinase 亚型特异性产品:

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Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NN-01-195 is a HSP90 inhibitor-drug conjugate. NN-01-195 binds tightly to and inhibits AURKA and HSP90, with an IC50 of 3.1 nM against AURKA and an IC50 of 8.7 nM against HSP90α. NN-01-195 induces mitotic arrest and spindle abnormality in tumor cells, and triggers cell apoptosis. NN-01-195 can be used in the research of solid tumors[1].

IC50 & Target[1]

HSP90α

8.7 nM (IC50)

体外研究
(In Vitro)

NN-01-195 (1-10000 nM) 可高效进入 HEK293T 细胞并与细胞内 HSP90 结合，未表现出明显的细胞通透性限制[1]。
NN-01-195 (0-10 μM; 24-72 hours) 可降低 FaDu 和 NCI-H1975 细胞活力，诱导 G2/M 期细胞周期阻滞、凋亡和有丝分裂纺锤体异常[1]。

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

NN-01-195 相关抗体:

Western Blot Analysis[1]

Cell Line: FaDu, NCI-H1975
Concentration: 500 and 1000 nM
Incubation Time: 72 h (cleaved PARP); 24 h (other targets)
Result: Induced cleaved PARP (a marker of apoptosis) in FaDu and NCI-H1975 cells.
Induced total AURKA expression and reduced p-AURKA levels in FaDu cells, did not alter HSP70 or HSP60 expression, and did not reduce p-S6, total S6, p-AKT, total AKT, p-ERK, or total ERK levels.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax T1/2 AUClast AUCinf
Mice[1] 10 mg/kg i.p. 0.500 h 9870 ng/mL 1.76 h 24114 ng·h/mL 26494 ng·h/mL
体内研究
(In Vivo)

NN-01-195 (10-80 mg/kg; i.p.; daily; 5 days) 在 C57BL/6J 小鼠中具有良好的耐受性，每日腹腔注射、连续给药 5 天的剂量最高可达 80 mg/kg，且无显著全身毒性[1]。
NN-01-195 (30 mg/kg; i.p.; daily; 14 days) 与 Adavosertib (HY-10993) 联合使用可对小鼠 FaDu 异种移植瘤的生长产生抑制作用[1]。
NN-01-195 (30 mg/kg; i.p.; daily; 21 days) 对小鼠 H1975 异种移植瘤生长具有抑制效果[1]。

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

Animal Model: NSG treated FaDu (6-10 weeks old, initial body weight 20-31 g)[1]
Dosage: 30 mg/kg (single-agent); 30 mg/kg (combination with 60 mg/kg adavosertib)
Administration: i.p.; daily; 14 days
Result: Did not cause a statistically significant reduction in tumor volume versus vehicle as a single agent.
Resulted in a statistically significant reduction in tumor volume versus vehicle, single-agent NN-01-195, single-agent adavosertib, and the VIC-1911 plus adavosertib combination when used in combination with adavosertib.
Led to a significantly lower Ki-67 H-score in tumor tissue in the NN-01-195 plus adavosertib group versus vehicle.
Caused no significant changes in body weight in any treatment group.
Animal Model: NSG treate H1975 (6-10 weeks old, initial body weight 20-31 g)[1]
Dosage: 30 mg/kg (single-agent); 30 mg/kg (combination with 60 mg/kg Adavosertib)
Administration: i.p.; daily; 21 days
Result: Showed slightly better quantitative control of tumor growth versus VIC-1911 as a single agent, but this did not reach statistical significance.
Provided good tumor growth control when used in combination with adavosertib.
Caused no significant changes in body weight in any treatment group.
分子量

1128.05

Formula

C56H60Cl2F4N12O5
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

NN-01-195 相关分类

  • 摩尔计算器

  • 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:

NN-01-195HSPAurora KinaseApoptosisHeat shock proteinsnon-small cell lung carcinomahead and neck squamous cell carcinomaNCI-H1975 non-small cell lung carcinoma cellsHSP90MRC5 fibroblastsHEK293T cellsmelanomasolid tumorsInhibitorinhibitorinhibit

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目录号：
HY-181626
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