ADSS2-IN-1
ADSS2-IN-1 is a ADSS2 inhibitor. ADSS2-IN-1 inhibits de novo AMP biosynthesis by targeting ADSS2, downregulates AMPK activity and promotes mitophagy in drug-resistant cells. ADSS2-IN-1 alone induces mild apoptosis in acute myeloid leukemia cells, and acts synergistically with BH3 mimetics to enhance the apoptotic effect. ADSS2-IN-1 restores the sensitivity of drug-resistant acute myeloid leukemia cells and reduces disease burden in immunocompetent mouse models. ADSS2 antagonist-1 can be used for the research of acute myeloid leukemia.
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- CAS No.: 375394-74-4
- 화학식: C11H11N5
- 분자량:213.24
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
In Vitro
ADSS2-IN-1 exhibits strong synergistic activity with BH3 mimetics (Venetoclax or S63845 (HY-100741)) in P4 acute myeloid leukemia (AML) cells, with a ZIP synergy score > 10, but shows no synergistic effect with the menin inhibitor Ziftomenib (HY-132001)[1].
ADSS2-IN-1 (2.5-10 μM; 72 h) enhances the Venetoclax-mediated reduction in cell viability and decreases the IC50 of Venetoclax when co-treatmented MA9/p53-KD mouse AML cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BH3 mimetic-resistant acute myeloid leukemia (AML) cell lines (P1-R, P2-R, P3-R cells)
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Synergistically eliminated BH3 mimetic-resistant P1-R, P2-R, and P3-R AML cells when combined with Venetoclax.
Showed minimal effect on cell viability when used alone.
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Cell Line:Double-hit murine AML cells (MA9/p53-KD cells)
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:72 h
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Result:Enhanced Venetoclax-mediated reduction of cell viability in MA9/p53-KD cells when co-treated with Venetoclax.
Lowered the Venetoclax IC50 value in MA9/p53-KD cells when co-treated with Venetoclax.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 CD45.1 (male and female, non-irradiated wild-type recipients injected with MA9/p53-KD cells)[1]
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Dosage:100 mg/kg
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Administration:i.p.; once daily; 5 consecutive days; 3 weeks
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Result:Reduced leukemia burden as measured by bioluminescent radiance (short-term 5-day treatment).
Modestly increased total and CD69+ T cells in bone marrow (short-term 5-day treatment).
Reduced leukemia burden measured by bioluminescent radiance (long-term 3-week treatment).
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Animal Model:C57BL/6 (male and female, wild-type)[1]
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Dosage:100 mg/kg
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Administration:i.p.; once daily; 5 times per week; 4 weeks
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Result:Showed no significant changes in body weight.
Showed no significant changes in bone marrow hematopoietic progenitor or mature lineage cell frequencies.
Showed no detectable histology abnormalities in kidney, liver, and spleen.
Chemical Information
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CAS No. 375394-74-4
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Appearance Solid
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분자량 213.24
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화학식 C11H11N5
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Color Light brown to brown
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SMILES
CC1=NN(C(N)=C1)C2=NC3=C(N2)C=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (468.96 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (9.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (9.75 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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 | 4.6896 mL | 23.4478 mL | 46.8955 mL | 117.2388 mL |
| 5 mM | 0.9379 mL | 4.6896 mL | 9.3791 mL | 23.4478 mL | |
| 10 mM | 0.4690 mL | 2.3448 mL | 4.6896 mL | 11.7239 mL | |
| 15 mM | 0.3126 mL | 1.5632 mL | 3.1264 mL | 7.8159 mL | |
| 20 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8619 mL | |
| 25 mM | 0.1876 mL | 0.9379 mL | 1.8758 mL | 4.6896 mL | |
| 30 mM | 0.1563 mL | 0.7816 mL | 1.5632 mL | 3.9080 mL | |
| 40 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.9310 mL | |
| 50 mM | 0.0938 mL | 0.4690 mL | 0.9379 mL | 2.3448 mL | |
| 60 mM | 0.0782 mL | 0.3908 mL | 0.7816 mL | 1.9540 mL | |
| 80 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4655 mL | |
| 100 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1724 mL |
ADSS2-IN-1 Related Classifications
HY-W264185 Related Classifications
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