10058-F4 Chemical Structure

10058-F4 Chemical Structure
Molecular Weight: 249.35

Validation & Quality Control

Customer Product Validation(2)

Quality Control & MSDS

Product Information

  • Compare c-Myc Inhibitors
    Compare c-Myc Products
  • Research Area

Product Description

Biological Activity

Description 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression.
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. [1] 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. [2]
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.[3]

Protocol(Only for Reference)

Cell Assay: [1]

Cell lines HL-60, U937, and NB-4 cells
Concentrations 0, 30, 60, 90, 120, 150 μM
Incubation Time 72 h
Method Cells, plated in 96-well plates (105/mL for cell lines and 5 × 105/mL for primary leukemic cells), are treated in triplicate with indicated concentrations of 10058-F4. At various time points, 20 μL 5 mg/mL MTT is added to each well. After incubation at 37°C for 3 hours, the MTT medium is removed and 100 μL DMSO lysis buffer is added. The number of viable cells is assessed by the percentage of absorbance of treated cells relative to that of solvent controls, using 570-nm wavelength on a spectrophotometer.

Animal Study: [3]

Animal Models PC-3 and DU145 xenografted SCID mice
Dosages 20 or 30 mg/kg
Administration i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Huang MJ, et al. Exp Hematol, 2006, 34(11), 1480-1489.

[2] Lin CP, et al. Anticancer Drugs, 2007, 18(2), 161-170.

view more

Chemical Information

Download 10058-F4 SDF
Molecular Weight (MW) 249.35


CAS No. 403811-55-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 50 mg/mL (200.52 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4-Thiazolidinone, 5-[(4-ethylphenyl)methylene]-2-thioxo

Customer Product Validation (2)

Click to enlarge
Source Cancer Discov, 2015, 5(9): 944-59. 10058-F4 purchased from Selleck
Method Western Blot
Cell Lines BT474 cells
Concentrations 10 µM
Incubation Time 48 h
Results Using two MYC inhibitors of MYC-MAX dimerization, 10058-F4 and 10074-G5, not only did we observe a decrease of HOXB7 expression, but also a reduction of HER2 and ER target gene expression.

Click to enlarge
Source Mol Cancer Res, 2015, 13(4): 699-712 . 10058-F4 purchased from Selleck
Method NHEJ Assay
Cell Lines MOLM14 cells
Concentrations 30 µm
Incubation Time
Results MOLM14 cells depleted of c-MYC by chemical inhibition had a general reduction in the size of DNA deletions when compared with DMSO-treated cells.

Product Use Citation (3)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related c-Myc Products

  • Ro-3306

    RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

  • K-Ras(G12C) inhibitor 12

    K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).

  • ML141

    ML141 is a potent, selective and reversible non-competitive inhibitor of Rho family GTPase cdc42 with IC50 of 200 nM.

  • Y-27632 2HCl

    Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

  • Palbociclib (PD-0332991) HCl

    Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

    Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).

  • Alisertib (MLN8237)

    Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.

    Features:First orally available inhibitor of Aurora A.

  • Palbociclib (PD0332991) Isethionate

    Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

    Features:The 1st specific inhibitor for CDK4/6 to show promise in multiple cancers.

  • MK-1775

    MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.

    Features:The first reported Wee1 inhibitor.

  • BI 2536

    BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. It shows 4- and 11-fold greater selectivity against Plk2 and Plk3. Phase 2.

    Features:The first potent and selective Plk1 inhibitor that induces all hallmarks of Plk1 inhibition.

  • Dinaciclib (SCH727965)

    Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Phase 3.

Recently Viewed Items

Tags: buy 10058-F4 | 10058-F4 supplier | purchase 10058-F4 | 10058-F4 cost | 10058-F4 manufacturer | order 10058-F4 | 10058-F4 distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
Contact Us