Genistein (NPI031L; BIO-00; G2535; PTI G-4660; SIPI9764I)

Alias: NPI 031L; NPI031L; NPI-031L; BIO-300; G-2535; PTI-G-4660; SIPI-9764-I; PTIG-4660; SIPI-9764I; BIO300; G2535; PTIG4660; SIPI9764I; BIO 300; G 2535; PTI G 4660; SIPI 9764 I; PTIG 4660; SIPI 9764I; Genistein

Cat No.:V0571 Purity: ≥98%

COA Product Data Instructions for use SDS

Genistein (NPI031L; BIO-00; G2535; PTI G-4660; SIPI9764I) Chemical Structure CAS No.: 446-72-0
Product category: EGFR

This product is for research use only, not for human use. We do not sell to patients.

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Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Genistein (NPI-031L; BIO-300; G-2535; PTI-G-4660; SIPI-9764I), a naturally occuring isoflavonoid isolated from soy products, is a potent multi-kinase inhibitor with potential anticancer activity against various cancers. Additionally, it is a phytoestrogen with selective estrogen receptor modulator effects on the estrogen receptors. Numerous additional biological activities, like those of an anthelmintic and antioxidant, are also present.

Biological Activity I Assay Protocols (From Reference)

Targets

EGFR; topo II

ln Vitro

Genistein is an ATP competitive inhibitor. In whole cells, including platelets, lymphocytes, and a variety of cultured cells, as well as in isolated enzyme and receptor preparations, genistein inhibits tyrosine phosphorylation. Additionally, it prevents Topo II (topoisomerase II) from being inhibited and EGF-stimulated phosphorylation in cultured cells. In cultured A431 epidermoid carcinoma cells, genistein suppresses EGF-stimulated tyrosine phosphorylation. With respect to ATP, inhibition is competitive, but not with respect to substrate.[1] Genistein inhibits the mitogenic effect on NIH-3T3 cells that is mediated by thrombin, insulin, and EGF.[2] Genistein binds to estrogen and PPARγ receptors in addition to acting as an agonist at the GPR30 receptor. With a Ki of 5.7 μM, genistein functions as an agonist at the PPARγ receptor after binding to it as well.[3]

ln Vivo

Genistein exhibits chemopreventive effects on tumors that are endocrine-dependent, including those of the breast and prostate in adult animals. In a dose-dependent manner, genistein in the diet decreased the incidence of poorly differentiated prostatic adenocarcinomas and down-regulated the mRNA expressions of the progesterone receptor, estrogen receptor-alpha, androgen receptor, prodermal growth factor receptor, insulin-like growth factor-I, and extracellular signal-regulated kinase-1, but not those of the estrogen receptor-beta and transforming growth factor-alpha. By controlling particular sex steroid receptors and growth factor signaling pathways, dietary genistein guards against prostate and breast cancers.[4] In order to increase mouse survival, genistein combined with prostate tumor irradiation causes a greater inhibition of primary tumor growth and increases control of spontaneous metastasis to para-aortic lymph nodes. It is paradoxical that genistein therapy alone promotes lymph node metastasis.[5]

Animal Protocol

Mice: 1, 2, 4 mg/kg; i.p.

Mice: Balb/c male mice are used. Genistein is administered as follows: On days 1-30, Genistein once daily, interaperitoneally injecting. Morphine plus Genistein is administered as follows: On days 1-30, Genistein once daily plus morphine, interaperitoneally injecting (17, 18). The same volume of saline is administered. Mice are randomly divided into 8 groups (n=6). 1) Normal saline group (1 mL DW/daily); 2) Morphine treated group; 3) Genistein 1 mg/kg treated group; 4) Genistein 2 mg/kg treated group 5) Genistein 4 mg/kg treated group; 6) Morphine plus Genistein 1 mg/kg treated group; 7) Morphine plus Genistein 2 mg/kg treated group; 8) Morphine plus Genistein 4 mg/kg treated group.

Rats: Male 8-week-old Wistar rats (150-180g) are used. After one week acclimation, all rats are randomly divided into 8 groups with 10 rats per group and treated for 35 weeks as follows: (1) STD group is fed with rodent standard chow diet (STD); (2) STD-BPA group is fed with STD and administered with BPA (50 μg/kg/day); (3) STD-(BPA+G) group is fed with STD and administered with BPA (50 μg/kg/day) plus Genistein (10 mg/kg/day); (4) STD-G group is fed with STD and administered with Genistein (10 mg/kg/day); (5) HFD group received high-fat diet (HFD); (6) HFD-BPA group is fed with HFD and administered with BPA (50 μg/kg/day); (7) STD-(BPA+G) group is fed with HFD and administered with BPA (50 μg/kg/day) plus Genistein (10 mg/kg/day); (8) HFD-G group is fed with HFD and administrated with Genistein (10 mg/kg/day). All the male genitors are treated for 35 weeks consecutively. The details of BPA (50 μg/kg/day) and Genistein (10 mg/kg/day) treatment methods have been described previously: BPA is dissolved in corn oil and diluted with three stock solutions (20, 40, 80, and 120 μg/mL).

References

[1]. J Biol Chem . 1987 Apr 25;262(12):5592-5.

[2]. Biochem Pharmacol . 1990 Jan 1;39(1):187-93.

[3]. J Biol Chem . 2003 Jan 10;278(2):962-7.

[4]. J Nutr . 2002 Mar;132(3):552S-558S.

[5]. Radiat Res . 2006 Jul;166(1 Pt 1):73-80.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C15H10O5
Molecular Weight	270.24
Exact Mass	270.05
Elemental Analysis	C, 66.67; H, 3.73; O, 29.60
CAS #	446-72-0
Related CAS #	Genistein;446-72-0
Appearance	Solid powder
SMILES	C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
InChi Key	TZBJGXHYKVUXJN-UHFFFAOYSA-N
InChi Code	InChI=1S/C15H10O5/c16-9-3-1-8(2-4-9)11-7-20-13-6-10(17)5-12(18)14(13)15(11)19/h1-7,16-18H
Chemical Name	5,7-dihydroxy-3-(4-hydroxyphenyl)chromen-4-one
Synonyms	NPI 031L; NPI031L; NPI-031L; BIO-300; G-2535; PTI-G-4660; SIPI-9764-I; PTIG-4660; SIPI-9764I; BIO300; G2535; PTIG4660; SIPI9764I; BIO 300; G 2535; PTI G 4660; SIPI 9764 I; PTIG 4660; SIPI 9764I; Genistein
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~54 mg/mL (~199.8 mM)

Water: <1 mg/mL

Ethanol: ~2 mg/mL (~7.4 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 3.75 mg/mL (13.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 37.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 3 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 3 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 4: 5 mg/mL (18.50 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.7004 mL	18.5021 mL	37.0041 mL
	5 mM	0.7401 mL	3.7004 mL	7.4008 mL
	10 mM	0.3700 mL	1.8502 mL	3.7004 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01489813	Active Recruiting	Drug: Genistein Drug: Sugar pill	Bladder Cancer	Emory University	May 19, 2017	Phase 2
NCT04482595	Recruiting	Drug: BIO 300 Oral Suspension Drug: Placebo	COVID-19 Long COVID	Humanetics Corporation	November 11, 2020	Phase 2
NCT01985763	Completed	Drug: Genistein	Colon Cancer Rectal Cancer	Sofya Pintova	November 2013	Phase 1 Phase 2
NCT01982578	Completed	Dietary Supplement: Genistein Other: Placebo	Alzheimer's Disease	Fundación para la Investigación del Hospital Clínico de Valencia	September 1, 2017	Not Applicable
NCT02624388	Terminated	Drug: Genistein Drug: Placebo	Lymphoma Solid Tumor	University of Virginia	August 2016	Phase 2

Biological Data

Effects of genistein on osteogenesis in KS483 cells. J Biol Chem . 2003 Jan 10;278(2):962-7.
Effects of genistein on osteogenesis in mouse bone marrow cells. J Biol Chem . 2003 Jan 10;278(2):962-7.
Effects of genistein on adipogenesis in KS483 cells and in mouse bone marrow cells. J Biol Chem . 2003 Jan 10;278(2):962-7.