Cat. No.: HY-163607

SpiD3

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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).

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Pureté: 98.24%
CAS No.: 3033533-25-1
Formule: C₂₇H₂₂N₂O₆
Masse moléculaire:470.47

Stockage:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

SpiD3 Chemical Structure

CAS No.: 3033533-25-1

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform NF-κB :

Cellular Effect

Cell Line	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]

In Vitro

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.

Cell Cytotoxicity Assay^[1]

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
Concentration:

0.01 µM, 0.1 µM, 1 µM, 10 µM, 100 µM
Incubation Time:

72 h
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.

Apoptosis Analysis^[1]

Cell Line:

HG-3 cells, OSU-CLL cells
Concentration:

0.25 μM, 0.5 μM, 1 μM
Incubation Time:

24 h
Result:

Induced apoptosis as indicated by increased Annexin V+ cells and PARP cleavage.

Cell Cycle Analysis^[1]

Cell Line:

OSU-CLL cells
Concentration:

0.25 μM, 0.5 μM, 1 μM
Incubation Time:

48 h
Result:

Accumulated in the G0-G1-phase with a corresponding reduction in the G2-M population.

Western Blot Analysis^[1]

Cell Line:

HG-3 cells, OSU-CLL cells
Concentration:

0.5 μM, 1 μM, 2 μM
Incubation Time:

4 h
Result:

Inhibited eIF2α phosphorylation and 4E-BP1 phosphorylation at Ser56.

In Vivo

SpiD3 (10 mg/kg; i.v.; daily; for 3 days) reduces tumor burden in Eµ-TCL1 mice^[1].

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

Animal Model:

Male and female Eµ-TCL1 (background: C57BL/6J) transgenic mice (10.2 months) with evident leukemia in the blood^[1].
Dosage:

10 mg/kg (prodrug of SpiD3 (dimethylamino prodrug)
Administration:

Tail vein intravenous injection; daily; for 3 days
Result:

Resulted in a significant decrease in leukemia burden in the blood and spleen.

Chemical Information

CAS No. 3033533-25-1
Appearance Solid
Masse moléculaire 470.47
Formule C₂₇H₂₂N₂O₆
Color White to off-white
SMILES

O=C1OC2(CC1=C)C(N(CCCN3C(C4(C5=C3C=CC=C5)OC(C(C4)=C)=O)=O)C6=C2C=CC=C6)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1255 mL

10.6277 mL

21.2553 mL

5 mM

0.4251 mL

2.1255 mL

4.2511 mL

10 mM

0.2126 mL

1.0628 mL

2.1255 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Eiken AP, et al. Novel Spirocyclic Dimer, SpiD3, Targets Chronic Lymphocytic Leukemia Survival Pathways with Potent Preclinical Effects. Cancer Res Commun. 2024;4(5):1328-1343. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Voir tous les produits spécifiques à Isoform NF-κB

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SpiD3 Related Classifications

HY-163607 Related Classifications