SpiD3
Based on 1 Customer Validation
SpiD3, a spirocyclic dimer, is an anticancer agent. SpiD3 markedly inhibits malignant B-cell proliferation and suppressed NF-κB activation independent of TME-associated stimuli. SpiD3 induces apoptosis and inhibits protein synthesis in chronic lymphocytic leukemia cells. SpiD3 can be used for study of chronic lymphocytic leukemia (CLL).
For research use only. We do not sell to patients.
- Purity: 98.24%
- CAS No.: 3033533-25-1
- Formula: C27H22N2O6
- Molecular Weight:470.47
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.23 μM
Compound: SpiD3
|
Antiproliferative activity against human A2780 cells assessed as cell growth inhibition measured after 3 days by cell viability assay
Antiproliferative activity against human A2780 cells assessed as cell growth inhibition measured after 3 days by cell viability assay
|
[PMID: 35367592] |
| CCRF-CEM | GI50 |
0.38 μM
Compound: SpiD3
|
Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| HL-60(TB) | GI50 |
0.38 μM
Compound: SpiD3
|
Antiproliferative activity against human HL-60(TB) cells assessed as reduction in the net protein increase inhibition by SRB assay
Antiproliferative activity against human HL-60(TB) cells assessed as reduction in the net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| K562 | GI50 |
0.38 μM
Compound: SpiD3
|
Antiproliferative activity against human K562 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| MIA PaCa-2 | IC50 |
0.13 μM
Compound: SpiD3
|
Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition measured after 3 days by cell viability assay
Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition measured after 3 days by cell viability assay
|
[PMID: 35367592] |
| MOLT-4 | GI50 |
0.38 μM
Compound: SpiD3
|
Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| OVCAR-5 | IC50 |
0.09 μM
Compound: SpiD3
|
Antiproliferative activity against human OVCAR-5 cells assessed as cell growth inhibition measured after 3 days by cell viability assay
Antiproliferative activity against human OVCAR-5 cells assessed as cell growth inhibition measured after 3 days by cell viability assay
|
[PMID: 35367592] |
| RPMI-8226 | GI50 |
0.38 μM
Compound: SpiD3
|
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| SF-268 | GI50 |
1.76 μM
Compound: SpiD3
|
Antiproliferative activity against human SF-268 cells assessed as reduction in the net protein increase inhibition by SRB assay
Antiproliferative activity against human SF-268 cells assessed as reduction in the net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| SF-295 | GI50 |
1.76 μM
Compound: SpiD3
|
Antiproliferative activity against human SF-295 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human SF-295 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| SF-539 | GI50 |
1.76 μM
Compound: SpiD3
|
Antiproliferative activity against human SF-539 cells assessed as reduction in the net protein increase inhibition by SRB assay
Antiproliferative activity against human SF-539 cells assessed as reduction in the net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| SNB-19 | GI50 |
1.76 μM
Compound: SpiD3
|
Antiproliferative activity against human SNB-19 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human SNB-19 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| SNB-75 | GI50 |
1.76 μM
Compound: SpiD3
|
Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| SR | GI50 |
0.38 μM
Compound: SpiD3
|
Antiproliferative activity against human SR cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human SR cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
| U-251 | GI50 |
1.76 μM
Compound: SpiD3
|
Antiproliferative activity against human U-251 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
Antiproliferative activity against human U-251 cells assessed as cell growth inhibition by measuring reduction in net protein increase inhibition by SRB assay
|
[PMID: 35367592] |
SpiD3 (0.01-100 µM; 72 h) shows antiproliferative properties in CLL cell lines[1].
SpiD3 (0.25-1 µM; 24 h) induces apoptosis in CLL cell lines[1].
SpiD3 (0.25-1 µM; 48 h) causes CLL cells to accumulate in the G0-G1 phase, and the number of cells in the G2-M phase decreases accordingly[1].
SpiD3 (0.5-2 µM; 4 h) induces the unfolded protein response (UPR) and inhibits protein translation in CLL cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HG-3 cells, OSU-CLL cells ,TP53 mutant MEC1 and MEC2 CLL cells, and aggressive mantle cell lymphoma and double-hit/triple-hit (DH/TH) lymphoma B cells
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Concentration:0.01 µM, 0.1 µM, 1 µM, 10 µM, 100 µM
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Incubation Time:72 h
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Result:Showed IC50 values of 0.12 µM, 0.33 µM, 0.41 µM, 0.55 µM, and < 0.9 µM against HG-3 cells, OSU-CLL, MEC1, MEC2 and DH/TH lymphoma B cells, respectively.
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Cell Line:HG-3 cells, OSU-CLL cells
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Concentration:0.25 μM, 0.5 μM, 1 μM
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Incubation Time:24 h
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Result:Induced apoptosis as indicated by increased Annexin V+ cells and PARP cleavage.
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Cell Line:OSU-CLL cells
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Concentration:0.25 μM, 0.5 μM, 1 μM
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Incubation Time:48 h
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Result:Accumulated in the G0-G1-phase with a corresponding reduction in the G2-M population.
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Cell Line:HG-3 cells, OSU-CLL cells
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:4 h
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Result:Inhibited eIF2α phosphorylation and 4E-BP1 phosphorylation at Ser56.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female Eµ-TCL1 (background: C57BL/6J) transgenic mice (10.2 months) with evident leukemia in the blood[1].
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Dosage:10 mg/kg (prodrug of SpiD3 (dimethylamino prodrug)
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Administration:Tail vein intravenous injection; daily; for 3 days
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Result:Resulted in a significant decrease in leukemia burden in the blood and spleen.
Chemical Information
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CAS No. 3033533-25-1
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Appearance Solid
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Molecular Weight 470.47
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Formula C27H22N2O6
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Color White to off-white
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SMILES
O=C1OC2(CC1=C)C(N(CCCN3C(C4(C5=C3C=CC=C5)OC(C(C4)=C)=O)=O)C6=C2C=CC=C6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL (53.14 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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: ≥ 2.5 mg/mL (5.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (282 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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1255 mL | 10.6277 mL | 21.2553 mL | 53.1384 mL |
| 5 mM | 0.4251 mL | 2.1255 mL | 4.2511 mL | 10.6277 mL | |
| 10 mM | 0.2126 mL | 1.0628 mL | 2.1255 mL | 5.3138 mL | |
| 15 mM | 0.1417 mL | 0.7085 mL | 1.4170 mL | 3.5426 mL | |
| 20 mM | 0.1063 mL | 0.5314 mL | 1.0628 mL | 2.6569 mL | |
| 25 mM | 0.0850 mL | 0.4251 mL | 0.8502 mL | 2.1255 mL | |
| 30 mM | 0.0709 mL | 0.3543 mL | 0.7085 mL | 1.7713 mL | |
| 40 mM | 0.0531 mL | 0.2657 mL | 0.5314 mL | 1.3285 mL | |
| 50 mM | 0.0425 mL | 0.2126 mL | 0.4251 mL | 1.0628 mL |