AT133873X 积分

目录号: GC13414纯度: >99.50%同义词: AT13387,Onalespib

AT13387是一种小分子非安沙霉素类HSP90（热休克蛋白90）抑制剂，其作用机制是通过靶向AKT和ERK信号通路。

Cas No.: 912999-49-6

规格	价格	库存	数量
5mg	¥735.00	现货	1
10mg	¥1,082.00	现货	1
50mg	¥2,489.00	现货	1
100mg	¥4,557.00	现货	1
500mg	¥12,600.00	现货	1
1g	¥20,580.00	现货	1
10mM (in 1mL DMSO)	¥840.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

AT13387 is a small-molecule, non-ansamycin HSP90 (heat shock protein 90) inhibitor that acts by targeting the AKT and ERK signaling pathways^[1]. AT13387 inhibits tumor cell growth and migration and exerts synergistic anti-cancer effects when combined with radiotherapy^[2]. AT13387 is commonly used in the study of non-small cell lung cancer (NSCLC)^[3].

AT13387 (0.1 - 2.5µM, 72h) inhibited cell proliferation in glioblastoma cell lines in a dose-dependent manner (IC₅₀ ≤ 0.25μM). AT13387 (0.4µM, 24h) significantly inhibited the proliferation and angiogenic potential of glioma cells^[4].

AT13387 (5, 10mg/kg/day; 3 days; i.p.) significantly reduced tumor growth and prolonged both median and overall survival in the radiosensitive HCT116 human adenocarcinoma xenograft mouse model^[2].

References:
[1] Riess J W, Reckamp K L, Frankel P, et al. Erlotinib and onalespib lactate focused on EGFR exon 20 insertion non-small cell lung cancer (NSCLC): a California Cancer Consortium Phase I/II Trial (NCI 9878)[J]. Clinical lung cancer, 2021, 22(6): 541-548.
[2] Spiegelberg D, Abramenkovs A, Mortensen A C L, et al. The HSP90 inhibitor Onalespib exerts synergistic anti-cancer effects when combined with radiotherapy: an in vitro and in vivo approach[J]. Scientific Reports, 2020, 10(1): 5923.
[3] Mooradian M J, Cleary J M, Giobbie‐Hurder A, et al. Dose‐escalation trial of combination dabrafenib, trametinib, and AT13387 in patients with BRAF‐mutant solid tumors[J]. Cancer, 2023, 129(12): 1904-1918.
[4] Canella A, Welker A M, Yoo J Y, et al. Efficacy of onalespib, a long-acting second-generation HSP90 inhibitor, as a single agent and in combination with temozolomide against malignant gliomas[J]. Clinical Cancer Research, 2017, 23(20): 6215-6226.

AT13387是一种小分子非安沙霉素类HSP90（热休克蛋白90）抑制剂，其作用机制是通过靶向AKT和ERK信号通路^[1]。AT13387可抑制肿瘤细胞的生长和迁移，并与放射疗法联合使用时具有协同抗癌作用^[2]。AT13387常用于非小细胞肺癌（NSCLC）的研究^[3]。

AT13387（0.1 - 2.5µM，72小时）以剂量依赖的方式抑制胶质母细胞瘤细胞系的增殖（IC₅₀≤ 0.25µM)。AT13387（0.4µM，24小时）可显著抑制胶质瘤细胞的增殖和血管生成能力^[4]。

AT13387（5、10mg/kg/天，3天，腹腔注射）显著降低了放射敏感型HCT116人腺癌异种移植小鼠模型的肿瘤生长，并延长了中位生存期和总生存期^[2]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:
Cell lines	LN229, U251HF and A172 Glioblastoma cell lines
Preparation Method	LN229, U251HF and A172 cells were seeded into 96 well plates and exposed to vehicle control (DMSO) or increasing concentrations of AT13387 (0.1 - 2.5μM) for 72h. Cell viability was measured using the WST-1 assay as per manufacturer’s instructions.
Reaction Conditions	0.1 - 2.5µM, 72h
Applications	AT13387 inhibited cell proliferation in a dose-dependent manner, with an IC₅₀ ≤ 0.25μM.
Animal experiment [2]:
Animal models	Radiosensitive HCT116 human adenocarcinoma xenograft mouse model
Preparation Method	Female nu/nu Balb/c mice were housed under standard laboratory conditions and fed ad libitum. Tumor xenografts were formed by subcutaneous inoculation of approximately 1×10⁶ HCT116 cells suspended in 100μL serum free cell culture medium in the right posterior leg. After approximately 10 days tumors had established (> 80mm³) and the treatment schedule started. HCT116 xenografted mice were divided into the following treatment groups: (i) control (N = 10), (ii) radiotherapy (N = 10) 3 × 2 Gy, (iii) AT13387 (N = 10) 3 × 10mg/kg AT13387, (iiii) AT13387 and 3 × 10mg/kg combined with 3 × 2 Gy (N = 10), (iv) AT13387 3 × 5mg/kg (N = 10), (v) AT13387 3 × 5mg/kg combined with 3 × 2 Gy (N = 10). Mice were injected intraperitoneally with 100µL AT13387 or (controls and radiation groups) with 100µL 17.5% β-Cyclodextrin on day 1, 2, and 3. Radiotherapy was given 6h after the drug treatment, performed under anesthesia on day 1, 2, and 3. Tumor size was measured every day with a digital caliper and survival analysis was performed after reaching the study endpoint of 1000mm³ tumor size.
Dosage form	5, 10mg/kg/day; 3 days; i.p.
Applications	AT13387 significantly reduced tumor growth and prolonged both median and overall survival in the HCT116 mouse model.
References: [1] Canella A, Welker A M, Yoo J Y, et al. Efficacy of onalespib, a long-acting second-generation HSP90 inhibitor, as a single agent and in combination with temozolomide against malignant gliomas[J]. Clinical Cancer Research, 2017, 23(20): 6215-6226. [2] Spiegelberg D, Abramenkovs A, Mortensen A C L, et al. The HSP90 inhibitor Onalespib exerts synergistic anti-cancer effects when combined with radiotherapy: an in vitro and in vivo approach[J]. Scientific Reports, 2020, 10(1): 5923.

产品文档 Product Documents

Purity:>99.50%

COA SDS Data Sheet NMR

化学性质Chemical Properties

CAS 号

912999-49-6

同义词

AT13387,Onalespib

化学名

(2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone

SMILES

CC(C)C1=C(C=C(C(=C1)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C)O)O

分子式

C₂₄H₃₁N₃O₃

分子量

409.5 g/mol

溶解性

≥ 13.25 mg/mL in DMSO, ≥ 47.7 mg/mL in EtOH with ultrasonic

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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