JMV7048_product_DataBase

Bioactivity	JMV7048 is an effective PROTAC degrader targeting PXR (Pregnane X Receptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker)[1].
Target	Pregnane X Receptor (PXR)
Invitro	JMV7048 (5 µM, 24 小时) 对结肠癌、肝癌和胰腺癌细胞系的癌细胞生长具有抑制作用[1]。JMV7048 (5 µM, 48 小时) 可显著降低移植入裸鼠的 CPP1 细胞的致瘤性 (即降低裸鼠中肿瘤起始的频率)[1]。JMV7048 (5 µM, 48 小时) 降低 CPP1、CPP14 和 CPP19 细胞在非附着条件下形成球体的能力，表明 JMV7048 能够影响这些细胞的自我更新能力[1]。JMV7048 (5 µM, 48 小时) 处理显著降低了 HT29 细胞在化疗药物 (5-Fluorouracil (HY-90006) 和 SN38 (HY-13704)) 处理后的存活率，表明 JMV7048 可能增强了细胞对化疗药物的敏感性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> JMV7048 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	JMV7048 (25 mg/kg，静脉注射，1 天 1 次，每周 5 天，共 15 天) 在无胸腺裸鼠和 NOD/scid 小鼠中耐受性良好[1]。JMV7048 (25 mg/kg，静脉注射，1 天 1 次，持续 4 天或每周 5 天持续 2 周) 在 HT29 和 CCP1 来源的 NOD/scid 小鼠异种移植瘤模型中显示出降解 PXR 的活性[1]。联合使用 JMV7048 (25 mg/kg，静脉注射，1 天 1 次，每周 5 天，共 4 周 (HT29 细胞); 25 mg/kg，腹腔注射，1 天 2 次，每周 5 天，共 3 周 (CCP1 细胞)) 与化疗药物 (50mg/kg 5-Fluorouracil (HY-90006) + 25mg/kg Irinotecan (HY-16562)，腹腔注射，每周 2 次，3 或 4 周)，在 NOD/scid 小鼠异种移植 (LS174T 细胞) 模型中可以显著延缓肿瘤复发[1]。单次腹腔注射 (50 mg/kg) 或静脉注射 (25 mg/kg) 的给药方式能在血浆中实现充分的药物暴露水平，而口服灌胃 (50 mg/kg) 给药方式则显著低效[1]。药代动力学分析[1] JMV7048
CAS	2871774-88-6
Formula	C53H64N8O7S
Molar Mass	957.19
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]. Bansard L, et al. A potent agonist-based PROTAC targeting Pregnane X Receptor that delays colon cancer relapse[J]. 2024.

PeptideDB

JMV7048

CAS: 2871774-88-6 F: C53H64N8O7S W: 957.19