EXO1-IN-1
Based on 1 Customer Validation
EXO1-IN-1 is a human exonuclease 1 (EXO1) inhibitor (IC50 = 15.7 μM). EXO1-IN-1 inhibits DNA end resection, promotes the accumulation of DNA double-strand breaks, and triggers S-phase polyamylation. EXO1-IN-1 induces apoptosis (Apoptosis) in BRCA1-deficient breast cancer cells. EXO1-IN-1 suppresses the growth of BRCA1-deficient breast cancer xenografts. EXO1-IN-1 can be used in research related to BRCA1-deficient breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 1111188-09-0
- Formula: C25H27N3O4S
- Molecular Weight:465.56
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
EXO1-IN-1 (F684) (0-300 μM; overnight treatment) selectively induces replication-associated DNA double-strand breaks and S-phase poly (ADP-ribosylation) in BRCA1-deficient MDA-MB-436 cells[1].
EXO1-IN-1 (20-40 μM; incubated overnight) inhibits replication fork-associated DNA end resection in MDA-MB-231 cells[1].
EXO1-IN-1 (0-100 μM; 48 h) inhibits homology-directed repair of site-specific double-strand DNA breaks (DSBs) and reduces HR frequency in U2OS cells[1].
EXO1-IN-1 (5-50 μM; 5 days) selectively induces apoptosis in BRCA1-deficient human breast cancer cell line MDA-MB-436[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BRCA1-deficient MDA-MB-436 cells
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Concentration:10, 50 μM
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Incubation Time:overnight
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Result:Increased the level of DNA damage, elicited a significant increase in γ-H2AX after 24 h.
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Cell Line:BRCA1-deficient MDA-MB-436 cells
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Concentration:0, 50, 100, 200, 300 μM
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Incubation Time:overnight
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Result:Increased the level of DNA damage, elicited a significant increase in γ-H2AX.
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Cell Line:MDA-MB-231 cells
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Concentration:20, 40 μM
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Incubation Time:overnight
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Result:Reduced the CPT-induced P-RPA levels
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Cell Line:BRCA1-/+ deficient MDA-MB-436 cells
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Concentration:5, 12, 25, 50 μM
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Incubation Time:5 days
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Result:Displays a
substantially stronger killing effect in a BRCA1− context.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (NOD SCID gamma) (6 to 8 week old male or female; xenograft model)[1]
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Dosage:8.5 mg/kg
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Administration:i.p.; daily; 20 days
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Result:Reduced the average growth rate of BRCA1− tumors.\n
Showed no significant effect on the average growth rate of BRCA1+ tumors.\n
Lowered normalized tumor volume significantly in BRCA1− tumors compared to vehicle controls over the course of the study.\n
Showed no significant difference in normalized tumor volume in BRCA1+ tumors compared to vehicle controls.
Chemical Information
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CAS No. 1111188-09-0
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Appearance Solid
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Molecular Weight 465.56
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Formula C25H27N3O4S
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Color White to off-white
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SMILES
CC1=C(N2CCN(C3=CC=C(NS(=O)(C4=CC=CC=C4)=O)C(C(O)=O)=C3)CC2)C=CC=C1C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (214.80 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)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.1480 mL | 10.7398 mL | 21.4795 mL | 53.6988 mL |
| 5 mM | 0.4296 mL | 2.1480 mL | 4.2959 mL | 10.7398 mL | |
| 10 mM | 0.2148 mL | 1.0740 mL | 2.1480 mL | 5.3699 mL | |
| 15 mM | 0.1432 mL | 0.7160 mL | 1.4320 mL | 3.5799 mL | |
| 20 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6849 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8592 mL | 2.1480 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7900 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0740 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8950 mL | |
| 80 mM | 0.0268 mL | 0.1342 mL | 0.2685 mL | 0.6712 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5370 mL |
EXO1-IN-1 Related Classifications
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