| Bioactivity | Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC)[1][2][3][4]. |
| Invitro | Onalespib lactate (0-0.4 µM; 72 h, 48 h) 抑制神经胶质瘤细胞的增殖、存活和迁移[2]。Onalespib lactate (0-0.4 µM; 48 h) 以剂量依赖性方式降低 EGFR、p-EGFR、AKT、P-AKT、ERK1/2、P-ERK1/2、S6、P-S6 蛋白的表达[2]。 Cell Proliferation Assay[2] Cell Line: |
| In Vivo | Onalespib lactate (30 mg/kg；i.v.；一次) 可穿过血脑屏障 (BBB) 并在 6 周龄 ICR 小鼠中引起 HSP90 的持续抑制[2]。Onalespib lactate (0.5 µM；移植后 5 至 10 天) 和 TMZ (HY-17364) (10 µM) 可减少斑马鱼胚胎中的肿瘤生长并延长存活期[2]。Onalespib lactate (5、10 mg/kg 用于 HCT116 异种移植物，20 mg/kg 用于 A431 异种移植物；i.p.；每天一次，持续 3 天) 在 HCT116 和 A431 异种移植物中显示出抗肿瘤活性[3]。 Animal Model: |
| Name | Onalespib lactate |
| CAS | 1019889-35-0 |
| Formula | C27H37N3O6 |
| Molar Mass | 499.60 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Riess JW, 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). Clin Lung Cancer. 2021 Nov;22(6):541-548. [2]. Canella A, et al. Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomas. Clin Cancer Res. 2017 Oct 15;23(20):6215-6226. [3]. Spiegelberg D, et al. The HSP90 inhibitor Onalespib exerts synergistic anti-cancer effects when combined with radiotherapy: an in vitro and in vivo approach. Sci Rep. 2020 Apr 3;10(1):5923. [4]. Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53(16):5956-69. |
Onalespib lactate
CAS: 1019889-35-0 F: C27H37N3O6 W: 499.60
Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value
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