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Cat. No.: HY-151426

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Anticancer agent 83

Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI₅₀ value of 0.15 mM. Anticancer agent 83 reduces mitochondrial membrane potential and induces DNA damage to induces leukemia cells apoptosis.

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CAS No.: 904815-29-8
Formule: C₂₀H₁₉N₅OS
Masse moléculaire:377.46

Stockage:

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

Data Sheet (269 KB)

Anticancer agent 83 Chemical Structure

CAS No.: 904815-29-8

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

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human A549 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
BALB/3T3	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
HaCaT	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human HaCaT cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human HaCaT cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
HCT-116	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
HCT-116	GI₅₀	8.4 μM Compound: 4a	Antiproliferative activity against p53-deficient human HCT-116 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against p53-deficient human HCT-116 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
HEK293	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human HEK293 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human HEK293 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
HeLa	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human HeLa cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human HeLa cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
HL-60(TB)	GI₅₀	2.8 μM Compound: 4a	Antiproliferative activity against human HL-60(TB) cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human HL-60(TB) cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
HOP-92	GI₅₀	2.85 μM Compound: 4a	Antiproliferative activity against human HOP-92 cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human HOP-92 cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
Jurkat	GI₅₀	0.69 μM Compound: 4a	Antiproliferative activity against human Jurkat cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human Jurkat cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
K562	GI₅₀	5.4 μM Compound: 4a	Antiproliferative activity against human K562 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human K562 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
KB 3-1	GI₅₀	7.4 μM Compound: 4a	Antiproliferative activity against human KB 3-1 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human KB 3-1 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
LOX IMVI	GI₅₀	0.15 μM Compound: 4a	Antiproliferative activity against human LOX IMVI cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human LOX IMVI cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
MCF7	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
MDA-MB-231	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
NCI-H460	IC₅₀	28 nM Compound: 4a	Antiproliferative activity against human NCI-H460 cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human NCI-H460 cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
NCI-H522	GI₅₀	1.97 μM Compound: 4a	Antiproliferative activity against human NCI-H522 cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human NCI-H522 cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
RXF 393	GI₅₀	4.27 μM Compound: 4a	Antiproliferative activity against human RXF 393 cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human RXF 393 cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
SF-295	GI₅₀	2.71 μM Compound: 4a	Antiproliferative activity against human SF-295 cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human SF-295 cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
SK-OV-3	GI₅₀	10 μM Compound: 4a	Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
SR	GI₅₀	1.77 μM Compound: 4a	Antiproliferative activity against human SR cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human SR cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
THP-1	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human THP-1 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human THP-1 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]
TK-10	GI₅₀	3.21 μM Compound: 4a	Antiproliferative activity against human TK-10 cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human TK-10 cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
UO-31	GI₅₀	2.88 μM Compound: 4a	Antiproliferative activity against human UO-31 cells incubated for 48 hrs and measured by SRB assay Antiproliferative activity against human UO-31 cells incubated for 48 hrs and measured by SRB assay	[PMID: 35973342]
WM793	GI₅₀	>100 μM Compound: 4a	Antiproliferative activity against human WM793 cells incubated for 72 hrs and measured by MTT assay Antiproliferative activity against human WM793 cells incubated for 72 hrs and measured by MTT assay	[PMID: 35973342]

In Vitro

Anticancer agent 83 (compound 4a) (0.01-100 μM; 24 h) showing strong activity towards human colon carcinoma HCT116 p53^−/− cells with deletion of P53 gene (GI₅₀=8.4 μM), human epidermoid cervix carcinoma KB3-1 (GI₅₀=7.4 μM), human ovarian carcinoma Skov 3 cells (GI₅₀=10 μM), and human chronic myelogenous leukemia K562 cells (GI₅₀=5.4 μM)^[1].
Anticancer agent 83 (0.5 μM; 24 h) interrupts DNA stability and induction of apoptosis in Jurkat cells, and decreases mitochondrial membrane potential^[1].

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

Cell Viability Assay^[1]

Cell Line:

Human colon carcinoma HCT116 p53−/− cells with deletion of P53 gene, human epidermoid cervix carcinoma KB3-1, human ovarian carcinoma Skov 3 cells, and human chronic myelogenous leukemia K562 cells
Concentration:

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

24 hours
Result:

Inhibited cell viability in different cells with GI₅₀s of 8.4 M (HCT116 p53^−/−), 7.4 M (KB3-1), 10 M (Skov 3), and 5.4 M (K562), respectively.

Immunofluorescence^[1]

Cell Line:

Jurkat cells
Concentration:

0.5 μM
Incubation Time:

24 hours
Result:

Induced morphological changes (including apoptotic bodies, membrane blebbing, chromatin condensation), and DNA fragmentation in Jurkat T-cells.

Chemical Information

CAS No. 904815-29-8
Masse moléculaire 377.46
Formule C₂₀H₁₉N₅OS
SMILES

O=C(C1=C(C)N(C2=CC=C(C(C)C)C=C2)N=N1)NC3=CC=C(SC#N)C=C3
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (269 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]. Pokhodylo N, et al. Novel N-(4-thiocyanatophenyl)-1H-1,2,3-triazole-4-carboxamides exhibit selective cytotoxic activity at nanomolar doses towards human leukemic T-cells. Eur J Med Chem. 2022 Nov 5;241:114633. [Content Brief]

Calculators

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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.

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100 mg

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