Structure of 10058-F4
CAS No.: 403811-55-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
10058-F4 is a c-Myc inhibitor that disrupts c-Myc-Max dimerization and the transactivation of c-Myc target genes.
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CAS No. : | 403811-55-2 |
Formula : | C12H11NOS2 |
M.W : | 249.35 |
SMILES Code : | O=C1N=C(S)SC1=CC2=CC=C(CC)C=C2 |
MDL No. : | MFCD04969046 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H317-H319 |
Precautionary Statements: | P280-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
TMR cells | 10 μM | Reduced expression of HOXB7, HER2, and ER target genes | PMC4560624 | |
BT474 cells | 1, 5, 10, 50 μM | 48 h | Combined with trastuzumab, significantly reduced cell viability | PMC4560624 |
H1299 cells | 10 µM | 24 h | Inhibited MYC expression and increased p21 protein levels | PMC8363664 |
human mammary epithelial cells (hMECs) | 10μM | To investigate the effect of MYC inhibitor 10058-F4 on miR-18a expression, results showed that 10058-F4 significantly reduced miR-18a expression in hMECs cultured on stiff substrates. | PMC3981899 | |
Jurkat cells | 5 nM | 12 h | Inhibited c-Myc expression, reduced GLS1 and GLUD expression, impaired T cell activation and proliferation | PMC10131875 |
intestinal organoids | 20 μM or 40 μM | 24 h | increased the secretion of total GLP-1 and active GLP-1 in response to glucose, along with elevated Gcg mRNA levels | PMC9944847 |
intestinal organoids | 40 μM | 48 h | reduced ceramide production and secretion | PMC9944847 |
DU145 | 100 nM | 48 h | To evaluate the effect of MYC inhibitor 10058-F4 on the radiosensitivity of DU145 cells, results showed that 10058-F4 significantly increased the radiosensitivity of DU145 cells. | PMC8315064 |
LNCaP | 100 nM | 48 h | To evaluate the effect of MYC inhibitor 10058-F4 on the radiosensitivity of LNCaP cells, results showed that 10058-F4 had a minor effect on the radiosensitivity of LNCaP cells. | PMC8315064 |
intestinal organoids | 20 μM or 40 μM | 24 h or 48 h | Treatment with 10058-F4 increased Gcg mRNA levels in intestinal organoids and promoted the secretion of total GLP-1 and active GLP-1. | PMC9944847 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
NSG mice | BT474 cell xenograft model | intraperitoneal injection | 30 mg/kg | daily, for the duration of the treatment | Combined with trastuzumab, significantly inhibited tumor growth | PMC4560624 |
nude mice | MDA-MB-231/ADR xenograft model | intraperitoneal injection | 20 mg/kg | every 3 days for 3 weeks | The combination of 10058-F4 and DOX significantly slowed down the tumor growth rate in nude mice and reduced the tumor size and weight. | PMC9005717 |
Nile tilapia | Bacterial infection model | Intraperitoneal injection | 10 mg/kg | Administered on day 1, 3, 5, and 6 post-infection | Inhibited c-Myc expression, reduced GLS1 and GLUD expression, impaired T cell proliferation and cytotoxicity, increased infection mortality | PMC10131875 |
Mice | TPO-Cre/LSL-BrafV600E mice | Gastric gavage and intraperitoneal injection | 30 mg/kg | Once daily for 2 weeks | To investigate the effect of 10058-F4 on PRC2 components and H3K27me3 levels in BrafV600E-induced thyroid cancer mouse model, the results showed that 10058-F4 significantly reduced tumor volume and weight, and decreased the levels of PRC2 components and H3K27me3 | PMC5485424 |
mice | HFD-induced obesity and hepatic steatosis model | oral | 50 mg/kg | daily for 8 weeks | improved HFD-induced obesity, insulin resistance, hepatic steatosis and fibrosis, accompanied by increased GLP-1 and decreased ceramide levels in serum | PMC9944847 |
mice | high-fat diet-induced obesity and hepatic steatosis model | oral | 50 mg/kg | daily for 8 weeks | 10058-F4 treatment reduced and liver weight gain, improved insulin resistance, and reduced hepatic steatosis. | PMC9944847 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
4.01mL 0.80mL 0.40mL |
20.05mL 4.01mL 2.01mL |
40.10mL 8.02mL 4.01mL |
Tags: 10058-F4 | c-Myc | Autophagy | Myc | c-Myc inhibitor | transcription factor | Myc/Max heterodimer | dimerization | 403811-55-2
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Code | Phrase |
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P305 | IF IN EYES: |
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P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
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P410 + P403 | Protect from sunlight. Store in a well-ventilated place. |
P410 + P412 | Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF. |
P411 + P235 | Keep cool. |
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H260 | In contact with water releases flammable gases which may ignite spontaneously |
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H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
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H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
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H335 | May cause respiratory irritation |
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H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
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H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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