PFKL-IN-1
PFKL-IN-1 is an orally active PFKL inhibitor, with a human-derived IC50 value of 52.63 nM and a Kd of 0.24 μM. PFKL-IN-1 directly binds to PFKL and inhibits its enzymatic activity. PFKL-IN-1 inhibits glycolysis, induces apoptosis and suppresses cell proliferation in breast cancer cells. PFKL-IN-1 exhibits antitumor efficacy in mouse models and enhances the therapeutic effect of anti-PD-L1 agents. PFKL-IN-1 can be used in breast cancer-related research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C39H29BrCl4F6N4S
- 分子量:921.45
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
hPFKL 52.63 nM (IC50) |
hPFKL 0.24 μM (Kd) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
1.05 μM
|
Antiproliferative activity against human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human MCF-7 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
|
42487371 |
| MDA-MB-231 | IC50 |
1.24 μM
|
Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
|
42487371 |
| MDA-MB-468 | IC50 |
0.85 μM
|
Antiproliferative activity against human MDA-MB-468 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human MDA-MB-468 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
|
42487371 |
| HCC1937 | IC50 |
0.87 μM
|
Antiproliferative activity against human HCC1937 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human HCC1937 breast cancer cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
|
42487371 |
PFKL-IN-1 (Compound 10w) (1-100 μM; 1 h pre-incubation with lysate prior to Pronase treatment) binds directly to PFKL in lysates of MCF-7 and MDA-MB-468 breast cancer cells[1].
PFKL-IN-1 (1-2 μM; 12-24 h) inhibits glycolysis in MCF-7 and MDA-MB-468 breast cancer cells in a PFKL-dependent manner, as evidenced by decreased levels of extracellular acidification rate (ECAR), glucose consumption and lactate production; this effect is completely abolished in PFKL-knockdown cells[1].
PFKL-IN-1 (24 h) inhibits the enzymatic activity of PFKL and reduces FBP levels in MCF-7 and MDA-MB-468 breast cancer cells, and its antiproliferative effect is partially mediated by this inhibition[1].
PFKL-IN-1 (48 h) potently inhibits the proliferation of MCF-7, MDA-MB-231, MDA-MB-468 and HCC1937 breast cancer cells, with IC50 values ranging from 0.85 to 1.24 μM after 48 h of treatment[1].
PFKL-IN-1 (1-4 μM; 48 h) inhibits DNA synthesis and proliferation of MCF-7 and MDA-MB-468 breast cancer cells[1].
PFKL-IN-1 (initial treatment for 48 h, followed by 14-day incubation) inhibits the clonogenic capacity of MCF-7 and MDA-MB-468 breast cancer cells in a dose-dependent manner after 48 h of treatment[1].
PFKL-IN-1 (0.25-1 μM; 48 h) inhibits the migration and invasion abilities of MCF-7 and MDA-MB-468 breast cancer cells in a dose-dependent manner[1].
PFKL-IN-1 (48 h) induces G0/G1 cell cycle arrest in MCF-7 and MDA-MB-468 breast cancer cells, which correlates with decreased protein levels of cyclin D1 and CDK4[1].
PFKL-IN-1 (1-4 μM; 48 h) induces apoptosis in MCF-7 and MDA-MB-468 breast cancer cells in a dose-dependent manner by upregulating the BAX/Bcl-2 ratio and activating caspase-3, and this effect depends on the expression of PFKL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7 and MDA-MB-468 breast cancer cells
-
Concentration:1, 2, 4 μM
-
Incubation Time:48 h
-
Result:Significantly reduced the number of EdU-positive cells in both MCF-7 and MDA-MB-468 cell lines, indicating inhibited DNA synthesis and cell proliferation.
-
Cell Line:MCF-7 and MDA-MB-468 breast cancer cells
-
Concentration:1, 2, 4 μM
-
Incubation Time:48 h
-
Result:Increased apoptotic rates in a dose-dependent manner in both cell lines.
Upregulated the BAX/Bcl-2 ratio and cleaved caspase-3 protein levels in a dose-dependent manner.
Did not further modulate apoptosis-related protein levels in PFKL-knockdown cells.
-
Cell Line:MCF-7 and MDA-MB-468 breast cancer cells
-
Concentration:0.25, 0.5, 1 μM
-
Incubation Time:48 h
-
Result:Significantly delayed wound closure in a dose-dependent manner in both cell lines, indicating reduced cell migratory capacity.
-
Cell Line:MCF-7 and MDA-MB-468 breast cancer cells
-
Concentration:0.25, 0.5, 1 μM
-
Incubation Time:48 h
-
Result:Reduced the number of invaded cells in a dose-dependent manner in both cell lines, indicating reduced invasive capacity.
| Species | Dose | Route | Tmax | T1/2 | Cmax | AUC0-t | AUC0-∞ | Vz | CL | MRT0-∞ | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 0.083 h | 7.424 h | 8767.998 ng/mL | 5236.117 ng·h/mL | 5496.937 ng·h/mL | 1943.597 mL/kg | 182.652 mL/h/kg | 2.641 h | / |
| Mice[1] | 10 mg/kg | p.o. | 2.500 h | 4.963 h | 182.809 ng/mL | 1478.485 ng·h/mL | 1203.429 ng·h/mL | / | / | 5.507 h | 2.8 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c mice (equal number of male and female)[1]
-
Dosage:25 mg/kg; 50 mg/kg
-
Administration:p.o.; daily; 14 days
-
Result:Achieved a tumor growth inhibition (TGI) rate of 21.4% at 25 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 59.5% at 50 mg/kg.
Caused no significant body weight loss in either treatment group.
Left serum levels of ALB, ALP, TG, CHO, and TP unchanged relative to controls.
Induced tumor necrosis in treated groups, with no pathological abnormalities detected in heart, liver, spleen, lung, or kidney.
Significantly reduced Ki67- and PCNA-positive proliferative cells in tumor tissues.
-
Animal Model:BALB/c mice[1]
-
Dosage:50 mg/kg
-
Administration:p.o.; daily; 12 days
-
Result:Enhanced the infiltration of CD8+ T lymphocytes and M1-polarized macrophages, while reducing M2-type macrophages in the tumor microenvironment when used alone.
Achieved a tumor growth inhibition (TGI) rate of 72.5% when combined with anti-PD-L1 antibody, compared to 40.5% with anti-PD-L1 monotherapy.
Caused no significant body weight changes during treatment.
化学情報
-
分子量 921.45
-
分子式 C39H29BrCl4F6N4S
-
SMILES
ClC1=C(CS/C(N[C@@H](CC2=CC=CC=C2)CN3C=[N+](C4=C3C=CC=C4)CC5=C(C=CC=C5Cl)Cl)=N\C6=CC(C(F)(F)F)=CC(C(F)(F)F)=C6)C(Cl)=CC=C1.[Br-]
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PFKL-IN-1 関連分類
HY-187532 関連分類
Powered by Bioz