SHetA2

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SHetA2 is a derivative of heteroarotinoid, that exhibits cytotoxicity in cancer cells with IC₅₀ of 0.37–4.6 μM. SHetA2 regulates cancer cells differentiation, induces apoptosis through the intrinsic mitochondrial pathway, and arrest cell cycle at G2 phase. SHetA2 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice. SHetA2 is orally active.

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SHetA2 Chemical Structure

CAS No. : 361483-66-1

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	2.98 μM Compound: 5, SHetA2	Growth inhibition of human A2780 cells after 72 hrs by MTS dye based cell titer-96 non-rad cell proliferation assay Growth inhibition of human A2780 cells after 72 hrs by MTS dye based cell titer-96 non-rad cell proliferation assay	[PMID: 25880346]
A2780	IC₅₀	3.17 μM Compound: SHetA2; NSC 721689	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter 96 non-radioactive cell proliferation assay Antiproliferative activity against human A2780 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter 96 non-radioactive cell proliferation assay	[PMID: 31831296]
A2780	IC₅₀	3.17 μM Compound: 1; SHetA2, NSC-721689	Antiproliferative activity against human A2780 cells assessed as reduction in cell growth after 72 hrs by CellTiter 96 Non-Rad cell proliferation assay kit method Antiproliferative activity against human A2780 cells assessed as reduction in cell growth after 72 hrs by CellTiter 96 Non-Rad cell proliferation assay kit method	[PMID: 30878829]
A2780	IC₅₀	3.17 μM Compound: NSC 721689, SHetA2; 1	Growth inhibition of human A2780 cells after 72 hrs by CellTiter-96 assay Growth inhibition of human A2780 cells after 72 hrs by CellTiter-96 assay	[PMID: 30245396]
DU-145	GI₅₀	3.47 μM Compound: SHetA2	Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25701251]
LNCaP	GI₅₀	2.25 μM Compound: SHetA2	Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25701251]
MCF7	GI₅₀	4.13 μM Compound: SHetA2	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25701251]
MDA-MB-453	GI₅₀	3.27 μM Compound: SHetA2	Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25701251]
PC-3	GI₅₀	4.8 μM Compound: SHetA2	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25701251]
T47D	GI₅₀	3.99 μM Compound: SHetA2	Cytotoxicity against human T47D cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human T47D cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 25701251]

Molecular Weight

401.55

Formula

C₂₀H₂₃N₃O₂S₂

CAS No.

361483-66-1

SMILES

S=C(NC1=CC=C([N+]([O-])=O)C=C1)NC2=CC3=C(SC(C)(CC3(C)C)C)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhang Y, et al., High performance liquid chromatographic analysis and preclinical pharmacokinetics of the heteroarotinoid antitumor agent, SHetA2. Cancer Chemother Pharmacol. 2006 Nov;58(5):561-9. [Content Brief]

[2]. Benbrook DM, et al., Flexible heteroarotinoids (Flex-Hets) exhibit improved therapeutic ratios as anti-cancer agents over retinoic acid receptor agonists. Invest New Drugs. 2005 Oct;23(5):417-28. [Content Brief]

SHetA2 Related Classifications

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SHetA2361483-66-1SHetA 2SHetA-2CaspaseReactive Oxygen SpeciesApoptosisCD2F1 mouseOVCAR3orally activeInhibitorinhibitorinhibit

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