2. Cell Cycle/DNA Damage Immunology/Inflammation NF-κB JAK/STAT Signaling Stem Cell/Wnt
  3. DNA/RNA Synthesis PD-1/PD-L1 IKK STAT STING
  4. XL-20

XL-20 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. XL-20 activates the cGAS-STING pathway. XL-20 upregulates the expression of PD-L1 in HR-deficient cancer cells. XL-20 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. XL-20 can be used in studies related to HR-deficient cancers.

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XL-20

XL-20 Chemical Structure

CAS No. : 3082173-75-6

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XL-20 Related Antibodies

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Description

XL-20 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. XL-20 activates the cGAS-STING pathway. XL-20 upregulates the expression of PD-L1 in HR-deficient cancer cells. XL-20 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. XL-20 can be used in studies related to HR-deficient cancers[1].

IC50 & Target[1]

Human pol θ

4.3 nM (IC50)

TBK1

 

STAT1

 

In Vitro

XL-20 (60 min) potently inhibits purified Polθ ATPase activity with an IC50 of 4.3 nM[1].
XL-20 (up to 80 μM; 7 days) potently inhibits the growth of HR-deficient MDA-MB-436, HCT116, and SW48 cells with IC50 values of 8.1 μM, 16.5 μM, and 17.2 μM respectively, and shows minimal activity in HR-proficient MDA-MB-231 cells (IC50 >80 μM)[1].
XL-20 (5-20 μM; 9 days) inhibits colony formation of MDA-MB-436 cells in a concentration-dependent manner[1].
XL-20 (5-20 μM; 7 days) induces apoptosis in MDA-MB-436 cells in vitro in a concentration-dependent manner[1].
XL-20 (5-20 μM; 7 days) induces concentration-dependent DNA double-strand break accumulation in MDA-MB-436 cells, as measured by γH2AX expression[1].
XL-20 (5-20 μM; 24 h) inhibits S-phase DNA synthesis in MDA-MB-436 cells in vitro in a concentration-dependent manner[1].
XL-20 (up to 10 μM) shows weak inhibition of the hERG potassium channel[1].
XL-20 (5-40 μM; 7 days) exhibits synergistic antiproliferative activity with Olaparib (HY-10162) in MDA-MB-436 cells, supporting a combination therapeutic strategy[1].
XL-20 (10 μM; 9-16 h) activates the cGAS-STING pathway in MDA-MB-436 cells, increasing phosphorylation of TBK1 and STAT1 and upregulating type I interferon-related genes and PD-L1, with stronger activity than AB25583 (HY-162859)[1].

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

XL-20 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: BRCA1-deficient MDA-MB-436 breast cancer cells
Concentration: 5, 10, 20 μM
Incubation Time: 9 days
Result: Inhibited colony formation in a concentration-dependent manner; at 20 μM, reduced relative colony formation to ~0.1.

Cell Proliferation Assay[1]

Cell Line: BRCA1-deficient MDA-MB-436 breast cancer cells
Concentration: 5, 10, 20 μM
Incubation Time: 24 h
Result: Inhibited S-phase DNA synthesis in a concentration-dependent manner; at 20 μM, reduced the percentage of EdU-positive cells.

Apoptosis Analysis[1]

Cell Line: BRCA1-deficient MDA-MB-436 breast cancer cells
Concentration: 5, 10, 20 μM
Incubation Time: 7 days
Result: Induced cell apoptosis in a concentration-dependent manner; at 20 μM, resulted in 17.7% apoptosis.
Parmacokinetics
Species Dose Route C0 AUC0-t AUC0-∞ T1/2 Vd CL MRT0-∞ Cmax Tmax Vd/F CL/F F
Rat[1] 1 mg/kg i.v. 5047.5 ng/mL 18622.7 ng·h/mL 19488.0 ng·h/mL 4.5 h 0.4 L/kg 0.06 L/h/kg 5.2 h / / / / /
Rat[1] 10 mg/kg i.g. / 256805.6 ng·h/mL 267456.2 ng·h/mL 5.1 h / / 7.3 h 29816.6 ng/mL 2.3 h 0.3 L/kg 0.04 L/h/kg 137.9 %
In Vivo

XL-20 (20 mg/kg; p.o.; daily; 12 days) monotherapy induces 43.7% tumor growth inhibition and increased DNA damage in MDA-MB-436 xenografts, while combination with olaparib (30 mg/kg; p.o.; daily; 12 days) enhances efficacy to 64% TGI with favorable tolerability[1].

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

Animal Model: BALB/C nude (female, 6-week-old, 18-20 g, subcutaneous xenograft of BRCA1-deficient human MDA-MB-436 breast cancer cells)[1]
Dosage: 20 mg/kg (monotherapy); 20 mg/kg + 30 mg/kg olaparib (combination)
Administration: p.o.; daily; 12 days
Result: Achieved a tumor growth inhibition (TGI) of 43.7%.
Increased γH2AX expression in tumor tissues compared to controls.
Showed no appreciable body weight loss.
Showed no significant drug-related toxicity via H&E staining of heart, liver, spleen, lung, and kidney.
Achieved a tumor growth inhibition (TGI) of 64% when combined with olaparib.
Increased γH2AX expression in tumor tissues to a greater extent than monotherapy compared to controls.
Molecular Weight

522.39

Formula

C24H18FN5O3Se
CAS No.
SMILES

COC1=CC=CC(F)=C1C2=C(C=NC(C)=C2)C(NC3=NN=C([Se]3)COC4=CC=C(C=C4)C#N)=O
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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XL-20 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:

XL-203082173-75-6XL20XL 20DNA/RNA SynthesisPD-1/PD-L1IKKSTATSTINGPD-1/Programmed death-ligand 1IκB kinaseI kappa B kinase Stimulator of Interferon GenesTMEM173MITAERISMPYSPolθ ATPaseSW48 cellsMDA-MB-436 cellsHR-deficient cancersHCT116 cellsDNA polymerase thetacGAS-STING pathwayMDA-MB-231 cellsPD-L1TMEJ DNA repair pathwayInhibitorinhibitorinhibit

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