2. PROTAC
  3. PROTACs
  4. JMV7048

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).

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JMV7048 Chemical Structure

JMV7048 Chemical Structure

CAS No. : 2871774-88-6

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Based on 1 publication(s) in Google Scholar

JMV7048 Related Antibodies

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Description

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].

IC50 & Target

Pregnane X Receptor (PXR)
In Vitro

JMV7048 (5 µM, 24 h) inhibits the growth of cancer cells in colon cancer, liver cancer, and pancreatic cancer cell lines[1].
JMV7048 (5 µM, 48 h) significantly reduces the tumorigenicity of CPP1 cells implanted in nude mice (i.e., decreases the frequency of tumor initiation in nude mice)[1].
JMV7048 (5 µM, 48 h) reduces the ability of CPP1, CPP14, and CPP19 cells to form spheres under non-adherent conditions, indicating that JMV7048 affects the self-renewal capability of these cells[1].
JMV7048 (5 µM, 48 h) treatment significantly decreases the survival rate of HT29 cells after treatment with chemotherapy drugs (5-Fluorouracil (HY-90006) and SN38 (HY-13704)), suggesting that JMV7048 may enhance the sensitivity of cells to chemotherapy drugs[1].

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

JMV7048 Related Antibodies

Western Blot Analysis[1]

Cell Line: LS174T cells (human colon adenocarcinoma); HepG2 (human hepatoma); AsPC-1 (human metastatic pancreatic adenocarcinoma), Human hepatocytes
Concentration: 0-5000 nM, 5 μM
Incubation Time: 24 h (0-5000 nM), 0-6 h (5 μM)
Result: Potently and efficiently reduced endogenous PXR protein in LS174T cells (0-5000 nM, 24 h or 5 μM, 0-6 h).
Significantly reduced the expression of PXR in HepG2 cells and AsPC-1 cells (at the dose of 5 μM, 24 h).
Failed to degrade PXR in primary cultures of human hepatocytes (at the dose of 5 μM, 24 h).

Cell Viability Assay[1]

Cell Line: LS174T cells, HT29 cells, CPP1 cells, CPP14 cells, CPP19 cells, CRC1 cells
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Resulted in no significant change in cell viability after 72 hours of treatment at concentrations as high as 20 μM, compared to treatment with the active metabolite of irinotecan (HY-16562) (SN38(HY-13704)).
In Vivo

JMV7048 (25 mg/kg, i.v., once daily, 5 days a week, for a total of 15 days) is well tolerated in athymic nude mice and NOD/scid mice[1].
JMV7048 (25 mg/kg, i.v., once daily, for 4 days or 5 days a week for 2 weeks) shows PXR degradation activity in HT29 and CCP1-derived NOD/scid mouse xenograft tumor models[1].
The combination of JMV7048 (25 mg/kg, i.v., once daily, 5 days a week, for 4 weeks (HT29 cells); 25 mg/kg, i.p., twice daily, 5 days a week, for 3 weeks (CCP1 cells)) with chemotherapy (50 mg/kg 5-Fluorouracil (HY-90006) + 25 mg/kg Irinotecan (HY-16562), i.p., twice a week, for 3 or 4 weeks) significantly delays tumor relapse in NOD/scid mouse xenograft (LS174T cells) models[1].
A single i.p. injection (50 mg/kg) or i.v. injection (25 mg/kg) achieves adequate drug exposure levels in plasma, while oral gavage (50 mg/kg) delivery is significantly less effective[1].

Pharmacokinetic Analysis in mice[1]

JMV7048 AUC (μg/L*h) Tmax (min) Cmax (μg/mL)
i.v. (25 mg/kg) 5.19 5 15.4
i.p. (30 mg/kg) 10.55 30 2
p.o. (25 mg/kg) 0.07 30 0.02

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

Animal Model: HT29 and CCP1-derived xenograft tumor models in NOD/scid mice
Dosage: 25 mg/kg
Administration: Intraperitoneal injection (i.p.), Intravenous injection (i.v.), 5 days a week
Result: Significantly delayed tumor relapse and extended tumor volume doubling time.
Animal Model: HT29 and CCP1-Derived Xenograft Tumor Models in NOD/scid Mice
Dosage: 25 mg/kg
Administration: Intravenous injection (i.v.), once daily for 4 days or 5 days a week for 2 weeks
Result: significantly reduced (approximately 50%) the expression of PXR in xenograft tumors, suggesting that JMV7048 maintains PXR-degrading activity in vivo.
Molecular Weight

957.19

Formula

C53H64N8O7S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(NC1=CC=C(N(CC2=CC=CC=C2)C(CCCCCCCNC(CCCCCN3CCN(C4=CC=C(C(N(C5CCC(NC5=O)=O)C6=O)=O)C6=C4)CC3)=O)=N7)C7=C1)(C8=C(C)C=C(C)C=C8C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (104.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0447 mL 5.2236 mL 10.4472 mL
5 mM 0.2089 mL 1.0447 mL 2.0894 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0447 mL 5.2236 mL 10.4472 mL 26.1181 mL
5 mM 0.2089 mL 1.0447 mL 2.0894 mL 5.2236 mL
10 mM 0.1045 mL 0.5224 mL 1.0447 mL 2.6118 mL
15 mM 0.0696 mL 0.3482 mL 0.6965 mL 1.7412 mL
20 mM 0.0522 mL 0.2612 mL 0.5224 mL 1.3059 mL
25 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0447 mL
30 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8706 mL
40 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6530 mL
50 mM 0.0209 mL 0.1045 mL 0.2089 mL 0.5224 mL
60 mM 0.0174 mL 0.0871 mL 0.1741 mL 0.4353 mL
80 mM 0.0131 mL 0.0653 mL 0.1306 mL 0.3265 mL
100 mM 0.0104 mL 0.0522 mL 0.1045 mL 0.2612 mL
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JMV7048 Related Classifications

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:

JMV70482871774-88-6JMV 7048JMV-7048PROTACsHT29 and CCP1-derived xenograft tumor models in NOD/scid miceLS174T cellsHepG2 cellsAsPC-1 cellsCancerInhibitorinhibitorinhibit

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