Cat. No.: HY-118474

GW 610

(Synonyms: NSC 721648)

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GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a K_i of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines.

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Pureté: 99.78%
CAS No.: 872726-44-8
Formule: C₁₅H₁₂FNO₂S
Masse moléculaire:289.32

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

GW 610 Chemical Structure

CAS No.: 872726-44-8

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Activité biologique
- Description
- Cellular Effect
- In Vitro
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 Cytochrome P450 :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	15.88 μM Compound: 1, PMX 610	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 22858144]
COLO 205	IC₅₀	13.94 μM Compound: 1, PMX 610	Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay	[PMID: 22858144]
HCC 2998	GI₅₀	0.00025 μM Compound: 8n	Antiproliferative activity against human colon cancer cell line HCC2998 Antiproliferative activity against human colon cancer cell line HCC2998	[PMID: 16392802]
HCC 2998	GI₅₀	0.25 nM Compound: 8n	Antiproliferative activity against human colon cancer cell line HCC2998 Antiproliferative activity against human colon cancer cell line HCC2998	[PMID: 16392802]
HCT-116	GI₅₀	5.4 μM Compound: 5	Antiproliferative activity against human HCT116 cell line Antiproliferative activity against human HCT116 cell line	[PMID: 16789754]
HT-29	GI₅₀	2.6 μM Compound: 5	Antiproliferative activity against human HT29 cell line Antiproliferative activity against human HT29 cell line	[PMID: 16789754]
KM12	GI₅₀	0.29 μM Compound: 8n	Antiproliferative activity against human colon cancer cell line KM12 Antiproliferative activity against human colon cancer cell line KM12	[PMID: 16392802]
MCF-10A	IC₅₀	25.22 μM Compound: 1, PMX 610	Cytotoxicity against human MCF10A cells after 24 hrs by MTT assay Cytotoxicity against human MCF10A cells after 24 hrs by MTT assay	[PMID: 22858144]
MCF7	GI₅₀	<0.0001 μM Compound: 8n	Antiproliferative activity against human breast cancer cell line MCF7 Antiproliferative activity against human breast cancer cell line MCF7	[PMID: 16392802]
MCF7	GI₅₀	<0.1 nM Compound: 8n	Antiproliferative activity against human breast cancer cell line MCF7 Antiproliferative activity against human breast cancer cell line MCF7	[PMID: 16392802]
MCF7	GI₅₀	0.008 μM Compound: 5	Antiproliferative activity against human MCF7 cell line Antiproliferative activity against human MCF7 cell line	[PMID: 16789754]
MCF7	GI₅₀	0.514 μM Compound: 5, PMX610, NSC-721648	Antiproliferative activity against human estrogen receptor positive MCF7 cells after 72 hrs by MTT assay in presence of aryl hydrocarbon receptor antagonist alpha-naphthoflavone Antiproliferative activity against human estrogen receptor positive MCF7 cells after 72 hrs by MTT assay in presence of aryl hydrocarbon receptor antagonist alpha-naphthoflavone	[PMID: 18666770]
MCF7	GI₅₀	<0.0001 μM Compound: 5, PMX610, NSC-721648	Antiproliferative activity against estrogen receptor positive human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against estrogen receptor positive human MCF7 cells after 72 hrs by MTT assay	[PMID: 18666770]
MCF7	GI₅₀	<0.1 nM Compound: 5, PMX610, NSC-721648	Antiproliferative activity against estrogen receptor positive human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against estrogen receptor positive human MCF7 cells after 72 hrs by MTT assay	[PMID: 18666770]
MCF7	IC₅₀	20.22 μM Compound: 1, PMX 610	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 22858144]
MDA-MB-468	GI₅₀	<0.0001 μM Compound: 8n	Antiproliferative activity against human breast cancer cell line MDA468 Antiproliferative activity against human breast cancer cell line MDA468	[PMID: 16392802]
MDA-MB-468	GI₅₀	<0.1 nM Compound: 8n	Antiproliferative activity against human breast cancer cell line MDA468 Antiproliferative activity against human breast cancer cell line MDA468	[PMID: 16392802]
MDA-MB-468	GI₅₀	<0.0001 μM Compound: 5	Antiproliferative activity against human MDA-MB-468 cell line Antiproliferative activity against human MDA-MB-468 cell line	[PMID: 16789754]
MDA-MB-468	GI₅₀	<0.1 nM Compound: 5	Antiproliferative activity against human MDA-MB-468 cell line Antiproliferative activity against human MDA-MB-468 cell line	[PMID: 16789754]
MDA-MB-468	GI₅₀	0.27 μM Compound: 5, PMX610, NSC-721648	Antiproliferative activity against estrogen receptor deficient human MDA468 cells after 72 hrs by MTT assay in presence of aryl hydrocarbon receptor antagonist alpha-naphthoflavone Antiproliferative activity against estrogen receptor deficient human MDA468 cells after 72 hrs by MTT assay in presence of aryl hydrocarbon receptor antagonist alpha-naphthoflavone	[PMID: 18666770]
MDA-MB-468	GI₅₀	<0.0001 μM Compound: 5, PMX610, NSC-721648	Antiproliferative activity against estrogen receptor deficient human MDA468 cells after 72 hrs by MTT assay Antiproliferative activity against estrogen receptor deficient human MDA468 cells after 72 hrs by MTT assay	[PMID: 18666770]
MDA-MB-468	GI₅₀	<0.1 nM Compound: 5, PMX610, NSC-721648	Antiproliferative activity against estrogen receptor deficient human MDA468 cells after 72 hrs by MTT assay Antiproliferative activity against estrogen receptor deficient human MDA468 cells after 72 hrs by MTT assay	[PMID: 18666770]

In Vitro

GW 610 inhibits the proliferation of MCF-7, MDA 468, KM 12, and HCC 2998 cells, with GI₅₀s of <0.1 nM, <0.1 nM, 290 nM, and 0.25 nM, respectively^[1].
GW 610 (0.1-1 μM) induces CYP1A1 mRNA and protein in MDA-MB-468, MCF-7, KM12, and HCC2998 cells, whereas CYP2S1 and CYP2W1 are induced only in breast cancer cells^[3].

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

Western Blot Analysis^[3]

Cell Line:

MDA-MB-468, MCF-7, KM12, and HCC2998 cells
Concentration:

0.1, 1 μM
Incubation Time:

48 hours
Result:

Induced CYP1A1 mRNA and protein in all cell lines including KM12 and HCC2998 CRC cells.
Induced CYP2S1 and CYP2W1 mRNA and protein expression in MDA-MB-468 and MCF-7 breast cancer cells.

Chemical Information

CAS No. 872726-44-8
Appearance Solid
Masse moléculaire 289.32
Formule C₁₅H₁₂FNO₂S
Color Light yellow to brown
SMILES

FC1=CC=C(SC(C2=CC=C(OC)C(OC)=C2)=N3)C3=C1
Synonyms

NSC 721648
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité

In Vitro:

DMSO : 25 mg/mL (86.41 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

3.4564 mL

17.2819 mL

34.5638 mL

5 mM

0.6913 mL

3.4564 mL

6.9128 mL

10 mM

0.3456 mL

1.7282 mL

3.4564 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 (protect from light). 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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.64 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 (273 KB)
SDS (251 KB)
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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]. Mortimer CG, et, al. Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines. J Med Chem. 2006 Jan 12;49(1):179-85. [Content Brief]

[2]. Aiello S, et, al. Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648). J Med Chem. 2008 Aug 28;51(16):5135-9. [Content Brief]

[3]. Tan BS, et, al. CYP2S1 and CYP2W1 mediate 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW-610, NSC 721648) sensitivity in breast and colorectal cancer cells. Mol Cancer Ther. 2011 Oct;10(10):1982-92. [Content Brief]

[4]. Boon Shing Tan, et al. CYP2S1 and CYP2W1 mediate 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW-610, NSC 721648) sensitivity in breast and colorectal cancer cells. Mol Cancer Ther. 2011 Oct;10(10):1982-92. [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	3.4564 mL	17.2819 mL	34.5638 mL	86.4095 mL
	5 mM	0.6913 mL	3.4564 mL	6.9128 mL	17.2819 mL
	10 mM	0.3456 mL	1.7282 mL	3.4564 mL	8.6410 mL
	15 mM	0.2304 mL	1.1521 mL	2.3043 mL	5.7606 mL
	20 mM	0.1728 mL	0.8641 mL	1.7282 mL	4.3205 mL
	25 mM	0.1383 mL	0.6913 mL	1.3826 mL	3.4564 mL
	30 mM	0.1152 mL	0.5761 mL	1.1521 mL	2.8803 mL
	40 mM	0.0864 mL	0.4320 mL	0.8641 mL	2.1602 mL
	50 mM	0.0691 mL	0.3456 mL	0.6913 mL	1.7282 mL
	60 mM	0.0576 mL	0.2880 mL	0.5761 mL	1.4402 mL
	80 mM	0.0432 mL	0.2160 mL	0.4320 mL	1.0801 mL

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GW 610

Antioxidant Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Voir tous les produits spécifiques à Isoform Cytochrome P450

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GW 610

Antioxidant Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Voir tous les produits spécifiques à Isoform Cytochrome P450

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GW 610 Related Classifications

HY-118474 Related Classifications