STF-1623
Based on 1 Customer Validation
STF-1623 is a highly potent, selective, cell-impermeable non-covalent ENPP1 inhibitor, with IC50 values of 0.6 nM and 800 nM against human ENPP1 and ENPP3, respectively. STF-1623 inhibits the hydrolysis of extracellular cGAMP by ENPP1, elevates intratumoral cGAMP levels, and indirectly enhances local cGAS-STING signaling and anti-tumor immunity in tumors. STF-1623 exhibits target-dependent retention in ENPP1-highly expressing tumors, while it undergoes rapid clearance in systemic circulation, and can penetrate into the CSF and brain parenchyma. STF-1623 can be used in studies related to breast cancer, pancreatic cancer, colorectal cancer, glioblastoma, and tumor immunology.
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- Pureté : 99.90%
- CAS No.: 2298391-60-1
- Formule: C16H22N3O4P
- Masse moléculaire:351.34
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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ENPP1 0.6 nM (IC50) |
ENPP3 800 nM (IC50) |
In Vitro
STF-1623 exhibits IC50 values of 0.6 nM and 800 nM against purified human ENPP1 and ENPP3, respectively, and shows over 1000-fold selectivity for ENPP1[3].
STF-1623 inhibits the hydrolysis of cGAMP by purified mouse ENPP1 with a Ki,app of 16 nM, and suppresses extracellular cGAMP degradation in cells expressing human ENPP1 with an IC50 of 68 nM[2].
STF-1623 exhibits extremely low membrane permeability in artificial membranes and cell membranes, confirming that it cannot penetrate cells[2].
Incubation with STF-1623 (2 μM; 16 h) for 16 h shows no toxicity to primary human PBMC[2].
STF-1623 does not inhibit any of the 468 tested kinases, exhibiting extremely high kinome selectivity[2].
STF-1623 (2 μM; 24 h) selectively increases extracellular cGAMP concentrations, whereas it does not affect intracellular cGAMP levels in ENPP1-/- 293T cGAS cells expressing human ENPP1 after 24 h of incubation[2].
STF-1623 (2 μM; 16 h) does not alter the gene expression of cytokines (IFNB1, CXCL10) in primary human PBMCs induced by electroporated cGAMP, with an incubation duration of 16 h[2].
Compared with the PBS control, STF-1623 (0.6 mM; 6-24 h) does not significantly induce extracellular cGAMP, IFN-β mRNA, or IFN-β secretion in RAW264.7 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 mouse macrophage cells
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Concentration:0.6 mM
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Incubation Time:24 h
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Result:Did not induce detectable extracellular cGAMP and induced only minimal IFN-β secretion.
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Cell Line:RAW264.7 mouse macrophage cells
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Concentration:0.6 mM
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Incubation Time:6 h
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Result:Did not significantly increase IFN-β mRNA compared with PBS.
In Vivo
STF-1623 (5-50 mg/kg; subcutaneous injection; once daily for 7 consecutive days) exerts effects in the orthotopic 4T1 breast cancer model: the 5 mg/kg dose delays primary tumor growth, while the 50 mg/kg dose improves the survival rate of mice[3].
STF-1623 (50-100 mg/kg; subcutaneous injection; once daily for 7 consecutive days) can cross the blood-brain barrier. When administered at a dose of 50 mg/kg in combination with temozolomide and ionizing radiation, it enables 62.5% of mice with intracranial GL261 glioblastoma to achieve complete tumor-free survival[3].
STF-1623 (50 mg/kg/day; subcutaneous injection; continuous administration; from day 0 to day 8) alone slows the growth of subcutaneous Panc02 tumors, and exerts a synergistic effect when combined with ionizing radiation, enhancing tumor growth inhibition and inducing disease stabilization or tumor regression in some mice[2].
STF-1623 (5-50 mg/kg; subcutaneous injection; once daily for 7 consecutive days, single-dose administration) increases intratumoral cGAMP levels and serum IFN−γ levels in an ENPP1-dependent manner[3].
STF-1623 (0.5-100 mg/kg; subcutaneous injection; once daily for 3 consecutive days, once daily for 7 consecutive days) combined with ionizing radiation reprograms the tumor immune microenvironment at doses ≥5 mg/kg, and completely inhibits the growth of Panc02 pancreatic tumors at doses of 50 or 100 mg/kg when combined with ionizing radiation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6 weeks old, orthotopic injection of 5-8 × 105 4T1 cells into the 4th mammary gland)[3]
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Dosage:5 mg/kg; 50 mg/kg
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Administration:s.c.; daily for 7 days
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Result:Delayed 4T1 primary tumor growth at 5 mg/kg.
Prolonged survival based on symptomatic metastatic disease at 50 mg/kg.
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Animal Model:BALB/c (female, 6 weeks old, subcutaneous injection of 3 × 106 Panc02 cells)[3]
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Dosage:0.5 mg/kg; 5 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:s.c.; daily for 3 days (days 1-3); s.c.; daily for 7 days (days 1-7)
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Result:Increased the intratumoral M1/M2 macrophage ratio, numbers of NK cells, NKT cells, CD4+ T cells, CD8+ T cells, and CD8+/Foxp3+ regulatory T cell ratio when combined with 15 Gy ionizing radiation at ≥5 mg/kg for ≥3 days.
Increased activated (CD69+, PD-1+) and proliferating (Ki67+) CD4+ and CD8+ T cells when combined with 15 Gy ionizing radiation at ≥5 mg/kg for ≥3 days.
Completely suppressed Panc02 tumor growth for over 30 days after treatment completion when combined with 20 Gy ionizing radiation at 50 or 100 mg/kg.
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Animal Model:C57BL/6 (intracranial injection of 3 × 105 GL261 Red-FLuc cells into the right frontal lobe)[3]
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Dosage:50 mg/kg (efficacy assessment); 100 mg/kg (blood-brain barrier assessment)
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Administration:s.c.; daily for 7 days (days 1-7); s.c.; single dose
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Result:Crossed the blood-brain barrier within 5 min at 100 mg/kg single dose, persisting above its IC95 (14 ng/g) at 24 h in cerebrospinal fluid and brain parenchyma.
Resulted in 62.5% (5/8) of mice being completely tumor-free on day 28 when combined with temozolomide and 15 Gy ionizing radiation at 50 mg/kg.
Exhibited superior survival compared to other treatment groups when combined with temozolomide and 15 Gy ionizing radiation at 50 mg/kg.
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Animal Model:C57BL6/J (female, 5-9 weeks old, subcutaneous implantation of 3 × 106 Panc02 cells)[2]
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Dosage:50 mg/kg/day
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Administration:s.c.; continuous; day 0 to day 8
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Result:Delayed Panc02 tumor growth.
Synergized with 20 Gy ionizing radiation to further delay tumor growth, with some mice achieving stable disease and tumor regression.
Chemical Information
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CAS No. 2298391-60-1
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Appearance Solid
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Masse moléculaire 351.34
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Formule C16H22N3O4P
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Color White to yellow
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SMILES
O=P(O)(O)CCC1CCN(C=2N=CN=C3C(OC)=CC=CC32)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (142.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (284 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Carozza JA, et al. Structure-Aided Development of Small-Molecule Inhibitors of ENPP1, the Extracellular Phosphodiesterase of the Immunotransmitter cGAMP. Cell chemical biology. 2020 Nov 19;27(11):1347-1358.e5. [Content Brief]
[2]. Carozza JA, et al. Extracellular cGAMP is a cancer cell-produced immunotransmitter involved in radiation-induced anti-cancer immunity. Nature cancer. 2020 Feb;1(2):184-196. [Content Brief]
[3]. Wang S, et al. ENPP1 inhibitor with ultralong drug-target residence time as an innate immune checkpoint blockade cancer therapy. Cell reports. Medicine. 2025 Sep 16;6(9):102336. [Content Brief]
[4]. Sun G, et al. Soft-Drug-Inspired MnSTF Nano-Adjuvant for Safe and Synergistic cGAS-STING Activation in Tumor Immunotherapy. Advanced science (Weinheim, Baden-Wurttemberg, Germany). 2026 Feb;13(9):e15432. [Content Brief]
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 |
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| DMSO | 1 mM | 2.8462 mL | 14.2312 mL | 28.4625 mL | 71.1561 mL |
| 5 mM | 0.5692 mL | 2.8462 mL | 5.6925 mL | 14.2312 mL | |
| 10 mM | 0.2846 mL | 1.4231 mL | 2.8462 mL | 7.1156 mL | |
| 15 mM | 0.1897 mL | 0.9487 mL | 1.8975 mL | 4.7437 mL | |
| 20 mM | 0.1423 mL | 0.7116 mL | 1.4231 mL | 3.5578 mL | |
| 25 mM | 0.1138 mL | 0.5692 mL | 1.1385 mL | 2.8462 mL | |
| 30 mM | 0.0949 mL | 0.4744 mL | 0.9487 mL | 2.3719 mL | |
| 40 mM | 0.0712 mL | 0.3558 mL | 0.7116 mL | 1.7789 mL | |
| 50 mM | 0.0569 mL | 0.2846 mL | 0.5692 mL | 1.4231 mL | |
| 60 mM | 0.0474 mL | 0.2372 mL | 0.4744 mL | 1.1859 mL | |
| 80 mM | 0.0356 mL | 0.1779 mL | 0.3558 mL | 0.8895 mL | |
| 100 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7116 mL |
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