1. Cell Cycle/DNA Damage
  2. G-quadruplex
  3. SOP1812

SOP1812 (QN-302) is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds to quadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer.

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SOP1812

SOP1812 Chemische Struktur

CAS. Nr. : 2546091-70-5

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Beschreibung

SOP1812 (QN-302) is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds to quadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer[1].

Cellular Effect
Cell Line Type Value Description References
BXPC-3 GI50
2.6 1
Compound: 11; SOP1812
Antiproliferative activity against human BxPC3 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human BxPC3 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
MIA PaCa-2 GI50
1.3 1
Compound: 11; SOP1812
Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
BXPC-3 GI50
2.6 1
Compound: 11; SOP1812
Antiproliferative activity against human BxPC3 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human BxPC3 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
CAPAN-1 GI50
5.9 1
Compound: 11; SOP1812
Antiproliferative activity against human Capan1 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human Capan1 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
PANC-1 GI50
1.4 1
Compound: 11; SOP1812
Antiproliferative activity against human PANC1 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human PANC1 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
CAPAN-1 GI50
5.9 1
Compound: 11; SOP1812
Antiproliferative activity against human Capan1 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human Capan1 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
MIA PaCa-2 GI50
1.3 1
Compound: 11; SOP1812
Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
BXPC-3 GI50
2.6 1
Compound: 11; SOP1812
Antiproliferative activity against human BxPC3 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human BxPC3 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
CAPAN-1 GI50
5.9 1
Compound: 11; SOP1812
Antiproliferative activity against human Capan1 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human Capan1 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
PANC-1 GI50
1.4 1
Compound: 11; SOP1812
Antiproliferative activity against human PANC1 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human PANC1 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
MIA PaCa-2 GI50
1.3 1
Compound: 11; SOP1812
Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
PANC-1 GI50
1.4 1
Compound: 11; SOP1812
Antiproliferative activity against human PANC1 cells assessed as growth inhibition after 96 hrs by SRB assay
Antiproliferative activity against human PANC1 cells assessed as growth inhibition after 96 hrs by SRB assay
[PMID: 32832034]
In Vitro

SOP1812 (0-50 nM; 96 h) inhibits the proliferation of many cancer cells[1].
SOP1812 (0-800 nM; 6-24 h) shows great affinity to hTERT G4 and HuTel21 G4[1].
SOP1812 (40 nM; 6-24 h) affects Wnt/β-catenin, axon guidance, Hippo, MAPK and Rap1 pathways[1].

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

Cell Proliferation Assay[1]

Cell Line: MIA PaCa-2, PANC-1, Capan-1 and BxPC-3 cell lines
Concentration: 0-50 nM
Incubation Time: 96 hours
Result: Showed anti-proliferation ability to MIA PaCa-2, PANC-1, Capan-1 and BxPC-3 cells with GI50 values of 1.3, 1.4, 5.9 and 2.6 nM, respectively.

Cell Viability Assay[1]

Cell Line: PANC-1 cells
Concentration: 0, 100, 400 and 800 nM
Incubation Time: 6 and 24 hours
Result: Binded to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively.

Cell Viability Assay[1]

Cell Line: MIA PaCa-2 Cells
Concentration: 40 nM
Incubation Time: 6 and 24 hours
Result: Affected WNT5B, DVL1, AXIN and APC2 expression which includes in Wnt/β-catenin pathway and also showed effects on axon guidance, Hippo, MAPK, and Rap1 pathways.
In Vivo

SOP1812 (1 mg/kg; i.v. once or twice per week for 28 days) shows anti-tumor activity in MIA PaCa-2 xenografts mice and KPC mice[1].

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

Animal Model: Female athymic nude mice with MIA PaCa-2 xenografts[1]
Dosage: 1 mg/kg
Administration: Intravenous injection; 1 mg/kg once or twice per week; for 28 days
Result: Showed complete tumor regression and no significant tumor regrowth after day 28 on several animals.
Animal Model: KPC mice with PDAC symptoms[1]
Dosage: 1 mg/kg
Administration: Intravenous injection; 1 mg/kg once per week; for 3 weeks
Result: Significantly extended survival of KPC mice and showed a better effect than gemcitabine.
Klinische Studie
Molekulargewicht

791.98

Formel

C45H57N7O6

CAS. Nr.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C1C2=CC(NCCN3CCCC3)=C4C(N(CCCN5CCOCC5)C(C6=CC(C7=CC=C(CN8CCCC8)C=C7)=C(C2=C64)C(N1CCCN9CCOCC9)=O)=O)=O

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Reinheit & Dokumentation
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