Cat. No.: HY-144898

SB-216

Customer Review

Based on 1 Customer Validation

SB-216 is an BBB-penetrable tubulin polymerization inhibitor. SB-216 can inhibit the proliferation and migration, and induce apoptosis and cell cycle arrest of tumor cells. SB-216 has good in vivo metabolic stability and low toxicity, but its oral bioavailability is limited. SB-216 has antitumor activity and can be used in the research of tumors such as melanoma.

For research use only. We do not sell to patients.

Purity: 99.93%
CAS No.: 2756818-39-8
Formula: C₁₇H₁₈N₄O₂
Molecular Weight:310.35

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

SB-216 Chemical Structure

CAS No.: 2756818-39-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: tubulin polymerization^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1.4 nM Compound: 5m	Antiproliferative activity against human A-375 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human A-375 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
A375/TxR	IC₅₀	1.1 nM Compound: 5m	Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
A549	IC₅₀	4.5 nM Compound: 5m	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
A549/TR	IC₅₀	2.8 nM Compound: 5m	Antiproliferative activity against human A549/Taxol cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human A549/Taxol cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
M14	IC₅₀	1.4 nM Compound: 5m	Antiproliferative activity against human M14 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human M14 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
MDA-MB-231	IC₅₀	4 nM Compound: 5m	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
MDA-MB-453	IC₅₀	0.5 nM Compound: 5m	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
MDA-MB-468	IC₅₀	1.8 nM Compound: 5m	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]
RPMI-7951	IC₅₀	1.5 nM Compound: 5m	Antiproliferative activity against human RPMI-7951 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Antiproliferative activity against human RPMI-7951 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34406768]

In Vitro

SB-216 (Compound 5m) (1-5 nM; 4-72 h) inhibits the viability of melanoma, breast cancer, and lung cancer cell lines (IC₅₀: 0.5-4.5 nM), and suppresses cell migration, induces apoptosis, and causes cell cycle arrest in A375/TxR cells^[1].

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

In Vivo

SB-216 (Compound 5m) (2-4 mg/kg; intravenous injection; twice weekly; 3 weeks) exhibits antitumor activity in a melanoma xenograft mouse model^[1].

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

Animal Model:

NSG mice aged 6-8 weeks old (225-250 g) treated A375/TxR melanoma cells^[1]
Dosage:

2 and 4 mg/kg
Administration:

Intravenous injection via tail vein, twice weekly for 3 weeks
Result:

Suppressed tumor growth throughout the study period.
Dose-dependently reduced spontaneous lung and liver metastases.
Had good tolerability in mice without obvious adverse reactions.

Chemical Information

CAS No. 2756818-39-8
Appearance Solid
Molecular Weight 310.35
Formula C₁₇H₁₈N₄O₂
Color White to off-white
SMILES

O=C1NC2=C(C=CC(OC)=C2)N(C3=C(CCC4)C4=NC(C)=N3)C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (201.39 mM; Need ultrasonic; 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

3.2222 mL

16.1108 mL

32.2217 mL

5 mM

0.6444 mL

3.2222 mL

6.4443 mL

10 mM

0.3222 mL

1.6111 mL

3.2222 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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: ≥ 2.08 mg/mL (6.70 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.70 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 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)
Handling Instructions (2659 KB)

References

[1]. Souvik Banerjee, et al. X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor. J Med Chem. 2021 Sep 9;64(17):13072-13095. [Content Brief]

[2]. Adeleye K L, et al. Abstract A019: Discovery of a potent and brain-penetrable tubulin inhibitor SB-216 that shows efficacy in primary tumor growth and brain metastasis. Molecular Cancer Therapeutics, 2024, 23(12_Supplement): A019-A019.

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

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
DMSO	1 mM	3.2222 mL	16.1108 mL	32.2217 mL	80.5542 mL
	5 mM	0.6444 mL	3.2222 mL	6.4443 mL	16.1108 mL
	10 mM	0.3222 mL	1.6111 mL	3.2222 mL	8.0554 mL
	15 mM	0.2148 mL	1.0741 mL	2.1481 mL	5.3703 mL
	20 mM	0.1611 mL	0.8055 mL	1.6111 mL	4.0277 mL
	25 mM	0.1289 mL	0.6444 mL	1.2889 mL	3.2222 mL
	30 mM	0.1074 mL	0.5370 mL	1.0741 mL	2.6851 mL
	40 mM	0.0806 mL	0.4028 mL	0.8055 mL	2.0139 mL
	50 mM	0.0644 mL	0.3222 mL	0.6444 mL	1.6111 mL
	60 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3426 mL
	80 mM	0.0403 mL	0.2014 mL	0.4028 mL	1.0069 mL
	100 mM	0.0322 mL	0.1611 mL	0.3222 mL	0.8055 mL

Keywords

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SB-216

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Cell Death Library

MCE Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SB-216

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Cell Death Library

MCE Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SB-216 Related Classifications

HY-144898 Related Classifications