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Art. -Nr.: HY-189234

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SAIT-PDZ-5179

SAIT-PDZ-5179 is a small-molecule inhibitor of GIPC1 that directly binds to the PDZ domain of GIPC1 with a K_D of 943 nM. SAIT-PDZ-5179 reduces the levels of GIPC1-associated signaling proteins and cell viability in pancreatic ductal adenocarcinoma models. SAIT-PDZ-5179 is used for studies on the GIPC1 signaling pathway and pancreatic ductal adenocarcinoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₃₀H₂₂FN₃O₄
Molecular Weight:507.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

SAIT-PDZ-5179 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

GIPC1

943 nM (Kd)

In Vitro

SAIT-PDZ-5179 (GIPCi) (GIPC1:GIPCi = 1:10; 2 h; 37 °C) interacts with the GIPC1 PDZ domain and induces local conformational stabilization in HDX-MS experiments, and the assay localizes the ligand-associated regions to include the 187-197 region and the adjacent regions of R279, D280, E282, and L283^[1].
SAIT-PDZ-5179 (GIPCi 7 μM; GIPC1 PDZ domain 76.4 μM; 25 °C; 90 s equilibration) binds to the GIPC1 PDZ domain in ITC experiments, with a K_D of 943 nM and a fitted stoichiometry N close to 1^[1].
SAIT-PDZ-5179 (10-50 μM; 72 h) reduces the protein levels of GIPC1, EGFR1, IGF1Rβ and SDC4 in KPC and PANC-1 cells in a concentration-dependent manner^[1].
SAIT-PDZ-5179 (10-50 μM; 72 h) reduces the viability of KPC, PANC-1, AsPC-1, and PANC-02 cells in a dose-dependent manner^[1].
SAIT-PDZ-5179 (5-50 μM; 72 h) reduces the viability of PDX-6741 and PDX-7114 pancreatic cancer cells in a dose-dependent manner^[1].
SAIT-PDZ-5179 (30 μM; followed by 21 days of colony growth) significantly reduces the clonogenic survival of PDX-6741 and PDX-7114 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

KPC; PANC-1
Concentration:

10-50 μM
Incubation Time:

72 h
Result:

Decreased GIPC1 protein expression in a concentration-dependent manner.
Decreased EGFR1 expression.
Decreased IGF1Rβ expression.
Decreased SDC4 expression.

Cell Viability Assay^[1]

Cell Line:

KPC; PANC-1; AsPC-1; PANC-02
Concentration:

10-50 μM
Incubation Time:

72 h
Result:

Reduced cell viability in a dose-dependent manner across all tested cell lines.

Cell Viability Assay^[1]

Cell Line:

PDX-6741; PDX-7114
Concentration:

5-50 μM
Incubation Time:

72 h
Result:

Reduced cell viability in a dose-dependent manner in both cell lines.

Cell Proliferation Assay^[1]

Cell Line:

PDX-6741; PDX-7114
Concentration:

30 μM
Incubation Time:

Colony growth: 21 days
Result:

Markedly reduced clonogenic survival in both cell lines.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_{INF_obs}	V_z	MRT_{INF_obs}	V_{ss_obs}
Mice^[1]	2 mg/kg	i.v.	755.4 ng/mL	0.033 h	7.71 h	3173.98 ng·h/mL	7011.4 mL/kg	9.63 h	6069.5 mL/kg

In Vivo

SAIT-PDZ-5179 (GIPCi) (2-10 mg/kg; i.p.; twice weekly for 3 consecutive weeks) dose-dependently reduces tumor volume and endpoint tumor weight in the KPC orthotopic pancreatic tumor mouse model^[1].
SAIT-PDZ-5179 (10 mg/kg; i.p.; twice weekly; for 3 consecutive weeks) reduces tumor volume and weight in the KPC orthotopic model, and extends median survival from 28 days in the control group to 43 days^[1].
SAIT-PDZ-5179 (10 mg/kg; i.p.; twice weekly; for 3 consecutive weeks) reduces tumor volume and weight and extends median survival from 32 days to 48 days in a PANC-1 orthotopic xenograft model^[1].
SAIT-PDZ-5179 (10 mg/kg; i.p.; twice weekly; for 3 consecutive weeks) reduces endpoint tumor volume and tumor weight in the PANC-1 subcutaneous xenograft model^[1].
SAIT-PDZ-5179 (10 mg/kg; i.p.; twice weekly; for 3 consecutive weeks) reduces tumor volume and tumor weight in the PDX-6741 orthotopic pancreatic tumor model^[1].
Combined intraperitoneal administration of SAIT-PDZ-5179 (10 mg/kg) and GEM (2 mg/kg), given twice weekly for 3 consecutive weeks, produces 78% tumor volume inhibition and 74% tumor weight inhibition in the KPC orthotopic model. These values exceed the Bliss-predicted inhibitions of 71.2% and 69.6%, corresponding to synergistic increases of 6.8% and 4.4%, respectively; the median survival of the combination treatment group is 46 days^[1].
Combined intraperitoneal administration of SAIT-PDZ-5179 (10 mg/kg) and GEM (2 mg/kg), given twice weekly for 3 consecutive weeks, produces 61% tumor volume inhibition and 84% tumor weight inhibition in the PANC-1 orthotopic xenograft model. These values are higher than the Bliss-predicted values of 59% and 58.18%, corresponding to synergistic increments of 2% and 25.82%, respectively; the median survival time of the combination treatment group is 54 days^[1].
Combined intraperitoneal administration of SAIT-PDZ-5179 (10 mg/kg) and GEM (2 mg/kg), given twice weekly for 3 consecutive weeks, produces 84% tumor volume inhibition and 79% tumor weight inhibition in the PDX-6741 orthotopic model. These values are higher than the Bliss-predicted inhibitions of 66.4% and 70.4%, corresponding to synergistic increments of 17.6% and 8.6%, respectively^[1].
SAIT-PDZ-5179 (10 mg/kg; i.p.; twice weekly; for 3 consecutive weeks) increases the infiltration of CD8⁺ and CD4⁺ T cells in KPC orthotopic tumors^[1].
SAIT-PDZ-5179 (10 mg/kg; i.p.; twice weekly for 3 consecutive weeks) does not induce histological abnormalities in the heart, kidney, liver, lung, or spleen, causes no significant body weight changes, and leads to no obvious alterations in serum ALT, AST, and KIM-1 levels in healthy SCID mice^[1].
SAIT-PDZ-5179 (5-25 mg/kg; single slow intravenous bolus injection; 14-day observation period) does not cause mortality in Sprague-Dawley rats at doses of 5-15 mg/kg, whereas 25 mg/kg results in acute death in 4 out of 6 animals after administration; surviving animals at 25 mg/kg exhibit transient somnolence and abdominal breathing, and recover on day 3^[1].

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

Animal Model:

SCID mice (female, 6-8 weeks old)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice weekly for 3 weeks
Result:

Reduced tumor volume.
Reduced tumor weight.
Prolonged median survival from 32 to 48 days.
Reduced Ki-67 and survivin staining.
Reduced EGFR1, integrin, and IGF1Rβ protein levels in tumor lysates.

Animal Model:

C57BL/6 mice (female, 6-8 weeks old, syngeneic orthotopic pancreatic ductal adenocarcinoma KPC model)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice weekly; 3 weeks
Result:

Reduced tumor volume.
Reduced tumor weight.
Prolonged median survival from 28 days in controls to 43 days.
Reduced tumor cellularity.
Reduced Ki-67 and survivin staining.
Increased intratumoral CD8⁺ T-cell infiltration.
Increased intratumoral CD4⁺ T-cell infiltration.
Reduced EGFR1, integrin, and IGF1Rβ protein levels in tumor lysates.

Animal Model:

SCID mice (female, 6-8 weeks old, subcutaneous PANC-1 pancreatic ductal adenocarcinoma xenograft model)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice weekly; 3 weeks
Result:

Significantly reduced tumor volume and tumor weight relative to control group animals, and mice exhibited no body weight loss.

Animal Model:

SCID mice (female, 6-8 weeks old, orthotopic PDX-6741 patient-derived pancreatic ductal adenocarcinoma model)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice weekly; 3 weeks
Result:

Produced marked reduction in tumor burden, with significant decreases in measured tumor volume and tumor weight corresponding to 66.4% tumor volume inhibition and 70.4% tumor weight inhibition relative to control.

Animal Model:

SCID mice (female, 6-8 weeks old, non-tumor bearing)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; twice weekly; 3 weeks
Result:

Showed no histopathological signs of toxicity in collected heart, kidney, liver, lung, and spleen tissues, no significant body weight variations were detected across the treatment period, and no elevations in serum ALT, AST, or KIM-1 biomarker levels were observed.

Animal Model:

7-8-week-old rats (Sprague-Dawley, male/female)^[1]
Dosage:

5, 10, 15, 25 mg/kg
Administration:

Single slow-bolus intravenous injection; 2 mL/kg; ≤1 mL/min; 14-day observation
Result:

Caused no mortality at 5, 10, or 15 mg/kg.
Caused acute mortality in 4 of 6 animals at 25 mg/kg.
Produced transient lethargy and abdominal breathing in surviving 25 mg/kg animals through day 2, with recovery by day 3.
Produced no compound-related hematological, coagulation, or serum biochemical alterations in surviving animals.
Produced no macroscopic lesions attributable to the compound.

Animal Model:

6–8-week-old mice (C57BL/6, female)^[1]
Dosage:

2, 5, 10 mg/kg
Administration:

i.p.;twice weekly for 3 weeks
Result:

Reduced tumor volume in a dose-dependent manner.
Reduced terminal tumor weight in a dose-dependent manner.

Chemical Information

Molecular Weight 507.51
Formel C₃₀H₂₂FN₃O₄
SMILES

OC1=C2C=CC=CC2=NC3=C1C=CC=C3/C(C4=CC=CC=C4)=C/C(NC5=CC(NC(OC)=O)=C(C=C5)F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Rachamala HK, et al. AI-driven discovery and validation of a GIPC1 PDZ domain inhibitor for pancreatic ductal adenocarcinoma. Cell reports. 2026 Jul 31.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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Minimum order quantity

100 mg

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