2. Protein Tyrosine Kinase/RTK
  3. c-Fms
  4. PXB17

PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC.

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PXB17 Chemical Structure

PXB17 Chemical Structure

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PXB17 Related Antibodies

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Description

PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC[1].

In Vitro

PXB17 (30 - 3000 nM; 4 h) dose-dependently can increase stability of CSF1R[1].
PXB17 (30, 100 nM; 24 h) halts cholesterol biosynthesis and prevent CRC development by blocking PI3K-AKT-mTORC1 signaling to induce conversion of the M2 phenotype to the M1 phenotype[1].
PXB17 (10, 30, 100 nM; 72 h) increases CD69 expression in CD8+ T cells. Also blocks CRC cell growth by enhancing anti-tumor immunity[1].

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

PXB17 Related Antibodies

Real Time qPCR[1]

Cell Line: BMDMs
Concentration: 10, 30, 100nM
Incubation Time: 24 h
Result: PXB17 shifted macrophages from an M2-like to an M1-like phenotype, indicated by changes in marker gene expression. The ability of PXB17 to reprogram macrophages suggests a role in enhancing anti-tumor immunity by converting immunosuppressive M2 macrophages into pro-inflammatory M1 macrophages, which are more capable of attacking tumor cells.

Immunofluorescence[1]

Cell Line: BMDMs
Concentration: 10, 30,100 nM
Incubation Time: 4 h
Result: PXB17 significantly inhibited CSF1R phosphorylation across all tested concentrations.
In Vivo

PXB17 (10, 20 mg/kg; p.o.; daily) effectively inhibits tumor growth in C57BL/6 mice were inoculated with MC-38 cell[1].
PXB17 (20 mg/kg ;p.o.; daily) not only influences tumor cell survival and proliferation by directly inhibiting CSF1R and modulating cholesterol biosynthesis pathways, but also remodels the tumor microenvironment by altering the phenotype of macrophages in C57BL/6, BALB/c mice were inoculated with MC-38 cell[1].
PXB17 (20 mg/kg ;p.o.; daily) Concomitant use with PD-1 mAb can improve anti-tumor efficacy and reduce recurrence in CT-26 (MSS), MC-38 (MSI-H) mice[1].

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

Animal Model: mice were inoculated with MC-38 cell [1]
Dosage: 10,20 mg/kg; daily
Administration: p.o.
Result: PXB17 significantly inhibited tumor growth and showed stronger anti-tumor effects at a dose of 20 mg/kg compared with PLX3397 (HY-16749). Meanwhile, tumor cell apoptosis was significantly increased in the PXB17-treated group, reprogramming of M2-type to M1-type macrophages, and enhanced activation and infiltration of CD8+ T cells.
Animal Model: mice were inoculated with CT-26 cell [1]
Dosage: 5, 10,20 mg/kg
Administration: p.o.
Result: PXB17 significantly inhibited CT-26 tumor growth at all doses. tumor tissues showed an increased proportion of M1-type macrophages, while decreasing the proportion of M2-type macrophages and enhancing CD8+ cell responses.
Molecular Weight

545.63

Formula

C29H35N7O4
SMILES

CC1=C(C(C)=C(N1)/C=C2C(NC3=C\2C=CC(NC(NC4=NOC(C(C)(C)C)=C4)=O)=C3)=O)NC(CN5CCCC5)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PXB17 Related Classifications

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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:

PXB17PXB 17PXB-17c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RColorectal cancerTumor associated macrophagesTumor immune microenvironmentCSF1R inhibitorAnti-PD-1 therapyCholesterol biosynthesisInhibitorinhibitorinhibit

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