2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  3. c-Fms PI3K
  4. JMC14

JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity.

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JMC14 Chemical Structure

JMC14 Chemical Structure

CAS No. : 2256080-83-6

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JMC14 Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity[1].

IC50 & Target

PI3Kα

389 nM (IC50)

PI3Kβ

890 nM (IC50)

PI3Kγ

＞10000 nM (IC50)

In Vitro

JMC14 (0-10 μM, 1 h) inhibits DLBCL cell proliferation via blocking PI3K-mediated signaling[1].
JMC14 (0.01-10 μM, 72 h) exerts potent anti-proliferative activity in M-NFS-60 cells by disrupting the CSF1/CSF1R signaling axis and its downstream pathways[1].
JMC14 (0.01-10 μM, 72 h) suppresses the proliferation of triple-negative breast cancer cells[1].

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

JMC14 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: M-NFS-60 myeloid leukemia cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 72 h
Result: Concentration-dependently inhibited the proliferation stimulated by CSF-1.
Had inhibitory potency on M-NFS-60 cell proliferation with IC50 values of 289 nM and 221 nM, respectively.

Cell Proliferation Assay[1]

Cell Line: TNBC 4T1, PY8119 and EMT6
Concentration: 0.1, 1, 10 μM
Incubation Time: 72 h
Result: Demonstrated moderate antiproliferative activity against all three cell lines, with IC50 values of 7.9 μM, 5.5 μM, or 6.5 μM, respectively.

Western Blot Analysis[1]

Cell Line: ABC-DLBCL TMD8 cells, GCB-DLBCL SU-DHL-6 and Pfeiffer cells
Concentration: 1 μM, 10 μM
Incubation Time: 1 h
Result: Suppressed AKT phosphorylation at S473 and T308 in a concentration-dependent manner.
Reduced AKT phosphorylation levels by approximately 40%.
Effectively inhibited the phosphorylation of downstream targets such as p70S6K1, 4E-BP1, and S6 at 1 μM.
Reduced AKT phosphorylation at S473 by 44.7%, while phosphorylation of p70S6K1 at T389 and S6 at S240/242 or S235/236 decreased by 39.7%, 55.4% or 50.6%, respectively at 10 μM.

Western Blot Analysis[1]

Cell Line: TMD8, SU-DHL-6, Pfeiffer
Concentration: 0, 0.01, 0.03, 0.1, 0.3, 1.0 μM
Incubation Time: 1 h
Result: Suppressed AKT phosphorylation at S473 and T308 in a concentration-dependent manner across all analyzed DLBCL cell lines.
Inhibited AKT phosphorylation by approximately 40% at 1 μM or 10 μM in TMD8 and Pfeiffer cells.

Western Blot Analysis[1]

Cell Line: TNBC 4T1, PY8119 and EMT6
Concentration: 0, 0.1, 0.3, 1, 10 μM
Incubation Time: 1 h
Result: Inhibited the phosphorylation of AKT, S6K, and S6, key signaling components downstream of PI3K, in a concentration-dependent manner.
was required to achieve similar levels to inhibit the phosphorylation of S6K and S6 compared to that of AKT with lower concentration.
Exerted lower potency in inhibiting Erk1/2 phosphorylation, achieving only 20% inhibition at a concentration of 10 μM.
In Vivo

JMC14 (10-100 mg/kg, p.o., once daily for 21 days) suppresses tumor growth in TMD8 xenografts and DLBCL PDX[1].
JMC14 (100 mg/kg, p.o., once daily for 13 days) displays potent activity via blocking CSF1R and PI3K signaling in M-NFS-60 myeloid leukemia model[1].
JMC14 (25-100 mg/kg, p.o., once daily for 18 days) attenuates the growth of PY8119 allografts and reprograms the TME[1].

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

Animal Model: TMD8 xenograft model (B-cell lymphoma), female Balb/c SCID mice[1]
Dosage: 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: p.o., once daily for 21 days
Result: Resulted in a dose-dependent inhibition of tumor growth.
Significantly inhibited the growth of xenografts with a T/C value of 17.6%.
Reduced significantly phosphorylated AKT at S473 1 h after administration at both 30 and 100 mg/kg.
Recovered phosphorylated AKT 8 h after treatment at 30 mg/kg, while inhibition of AKT phosphorylation persisted up to 8 h and was reversed up to 24 h upon treatment.
Significantly suppressed the growth of LY-24-0063 PDX, resulting in a T/C value of 35.2% at 100 mg/kg.
Exhibited marginal effect, with T/C values of 94.0% or 82.5%, respectively at 10 mg/kg or 30 mg/kg.
Animal Model: SCID mice bearing M-NFS-60 xenografts model[1]
Dosage: 100 mg/kg
Administration: p.o., once daily for 13 days
Result: Significantly suppressed tumor growth, yielding a T/C value of 25.4% at 100 mg/kg.
Observed no significant changes in body weight between treatment and control groups.
Decreased the anti-tumor effect correlated with the suppression of CSF1R and PI3K signaling pathways in the phosphorylation of CSF1R, Erk1/2, AKT, S6K and S6 in tumor tissues collected 2 h after a single dose.
Animal Model: Immune-competent model, PY8119 cells were orthotopically inoculated into C57BL/6 mice[1]
Dosage: 25, 50, 100 mg/kg
Administration: p.o., once daily for 18 days
Result: Inhibited the tumor growth in a dose-dependent manner.
Exhibited pronounced tumor growth inhibition with a T/C value of 26.9% at 100mg/kg.
Animal Model: Immune-competent model, PY8119 cells were orthotopically inoculated into C57BL/6 mice[1]
Dosage: 100 mg/kg
Administration: p.o., single dose, tumor tissues were collected at 2, 4, and 8 h after treatment.
Result: Effectively down-regulated the phosphorylation of CSF1R, AKT, S6K, and S6 within 2 h after administration, while a longer time was needed to suppress the Erk1/2 phosphorylation.
Recovered phosphorylation of AKT and S6 partially 8 h post-treatment.
Increased the staining CD45 markedly after treatment, indicating enhanced immune cell infiltration.
Decrease the F4/80 staining, the staining of CD206 representing immunosuppressive M2 macrophages significantly particularly.
Molecular Weight

533.59

Formula

C26H34F3N7O2
CAS No.
SMILES

OC(C1CCN(CC1)CC2=C(N3N=C(N=C(C3=C2)N4CCOCC4)C5=CN=C(C=C5C(F)(F)F)N)C)(C)C
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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JMC14 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:

JMC142256080-83-6JMC 14JMC-14c-FmsPI3KCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RPhosphoinositide 3-kinaseB cell malignancyTNBCM-NFS-60dual inhibitionInhibitorinhibitorinhibit

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