[CAS NO. 403811-55-2] 10058-F4

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PRODUCTS SPECIFICATIONS [403811-55-2]

Catalog

SLK-S7153

Brand

Selleck

CAS

403811-55-2

DESCRIPTION [403811-55-2]

Overview

MDL	MFCD04969046
Molecular Weight	249.35
Molecular Formula	C12H11NOS2
SMILES	C(=C1C(=O)NC(=S)S1)C2=CC=C(CC)C=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	4.0104 mL	20.0521 mL	40.1043 mL
5 mM	0.8021 mL	4.0104 mL	8.0209 mL
10 mM	0.4010 mL	2.0052 mL	4.0104 mL
50 mM	0.0802 mL	0.4010 mL	0.8021 mL

Description

10058-F4 is a inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent and modulates .

Targets

c-Myc ^[1]
(Cell-free assay)

In vitro

10058-F4 inhibits growth of leukemic cells and dimerization of Myc and Max. 10058-F4 induces cell-cycle arrest and apoptosis of AML cells. 10058-F4 arrests AML cells at G0/G1 phase, downregulates c-Myc expression and upregulated CDK inhibitors, p21 and p27. Meanwhile, 10058-F4 induces apoptosis through activation of mitochondrial pathway shown by downregulation of Bcl-2, upregulation of Bax, release of cytoplasmic cytochrome C, and cleavage of caspase 3, 7, and 9. Furthermore, 10058-F4 also induces myeloid differentiation, possibly through activation of multiple transcription factors. Similarly, 10058-F4-induced apoptosis and differentiation could also be observed in primary AML cells. 10058-F4 decreases c-Myc protein levels, inhibites proliferation of HepG2 cells likely through upregulation of cyclin-dependent kinase (cdk) inhibitor, p21WAF1 and lowers intracellular levels of [alpha]-fetoprotein (AFP). Treatment with 10058-F4 also downregulates human telomerase reverse transcriptase (hTERT) at the transcriptional level. In addition to inhibiting the proliferation of HepG2 cells, 10058-F4 enhances sensitivity to conventional chemotherapeutic agents, doxorubicin, 5-fluorouracil (5-FU) and cisplatin.

In vivo

Peak plasma 10058-F4 concentrations of approximately 300 μM are seen at 5 min and declined to below the detection limit at 360 min following a single iv dose. Plasma concentration versus time data are best approximated by a two-compartment, open, linear model. The highest tissue concentrations of 10058-F4 are found in fat, lung, liver, and kidney. Peak tumor concentrations of 10058-F4 are at least tenfold lower than peak plasma concentrations. Eight metabolites of 10058-F4 are identified in plasma, liver, and kidney. The terminal half-life of 10058-F4 is approximately 1 h, and the volume of distribution is >200 ml/kg. No significant inhibition of tumor growth is seen after i.v. treatment of mice with either 20 or 30 mg/kg 10058-F4.

References

[1] Huang MJ, et al. Exp Hematol, 2006, 34(11), 1480-1489.
[2] Lin CP, et al. Anticancer Drugs, 2007, 18(2), 161-170.
[3] Guo J, et al. Cancer Chemother Pharmacol, 2009, 63(4), 615-625.

Synonyms

4-Thiazolidinone, 5-[(4-ethylphenyl)methylene]-2-thioxo-

5-[(4-Ethylphenyl)methylene]-2-thioxo-4-thiazolidinone

10058F4