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| Targets |
Chromeceptin (94G6) is described as a synthetic small benzochrome derivative that inhibits the IGF (Insulin-like Growth Factor) signaling pathway in cancer, including hepatocellular carcinoma (HCC). [1]
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| ln Vitro |
Time-blocked inhibition of IGF2 expression in Hep3B TS cells is observed with chromeceptin (94G6) (5 μM) [1]. Rapamycin (mTOR) and protein regulatory B (AKT, Ser463 of AKT, TS cells) are both decreased by chromececeptin. The phosphorylation of the ser371 site in the mTOR effector ribosomal protein S6 rest (p70S6K) is inhibited by chromeceptin [1].
Treatment of Hep3B-derived tumorsphere (TS) cells with Chromeceptin inhibited IGF2 expression in a time-dependent manner. [1] Chromeceptin treatment decreased the number of spheres formed by Hep3B cells in a dose-dependent manner. [1] Chromeceptin treatment decreased the viability of Hep3B-derived TS cells in a dose-dependent manner. [1] In Hep3B-derived TS cells, Chromeceptin treatment decreased the phosphorylation levels of downstream signaling molecules: protein kinase B (AKT at Ser473) and mammalian target of rapamycin (mTOR at Ser2481 and Ser2448). It also repressed phosphorylation at Ser371 in the mTOR effector ribosomal protein S6 kinase (p70S6K). [1] Chromeceptin treatment suppressed the viability of TS cells derived from primary hepatocellular carcinoma cells of four HCC patients. [1] |
| Cell Assay |
Tumorsphere Formation Assay: Hep3B cells were cultured under tumorsphere (TS) culture conditions (in ultra-low attachment dishes with CSC culture medium) to enrich cancer stem cells. The sphere-forming ability was assessed after treatment with different concentrations of Chromeceptin. The number of spheres was enumerated by microscopic examination. [1]
Cell Viability Assay: The viability of tumorsphere (TS) cells after Chromeceptin treatment was estimated using a luminescent cell viability assay kit. Luminescence, proportional to the amount of ATP present (an indicator of metabolically active cells), was measured using a multilabel counter. [1] Immunoblot Analysis: Cells (2D adherent or TS cultures) treated with Chromeceptin were lysed. Proteins were resolved by SDS-PAGE, transferred to a membrane, and probed with specific antibodies against target proteins (e.g., IGF2, p-AKT, total AKT, p-mTOR, total mTOR, p-p70S6K). Beta-actin was used as a loading control. Proteins were visualized using enhanced chemiluminescence. This method was used to detect changes in IGF2 expression and phosphorylation status of signaling pathway components. [1] |
| References | |
| Additional Infomation |
Chromeceptin (94G6) is a compound previously reported to inhibit IGF2 mRNA and protein levels in hepatocytes and hepatocellular carcinoma cells. [1] In this study, Chromeceptin was used as a pharmacological tool to inhibit the IGF2 pathway. Data showed that IGF2 plays a role in maintaining cancer stem cell characteristics and tumor spheroid viability in Hep3B cells through the pAKT and p-mTOR pathways. [1]
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| Molecular Formula |
C19H16F3N3O
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|---|---|
| Molecular Weight |
359.3522
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| Exact Mass |
359.125
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| Elemental Analysis |
C, 63.51; H, 4.49; F, 15.86; N, 11.69; O, 4.45
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| CAS # |
331859-86-0
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| Related CAS # |
331859-86-0
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| PubChem CID |
3113922
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| Appearance |
White to light yellow solid powder
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| LogP |
4.689
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
607
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=C(C#N)C(C2C=CC=C(C(F)(F)F)C=2)C2C=CC(N(C)C)=CC=2O1
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| InChi Key |
GVINXTXGDDSXFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16F3N3O/c1-25(2)13-6-7-14-16(9-13)26-18(24)15(10-23)17(14)11-4-3-5-12(8-11)19(20,21)22/h3-9,17H,24H2,1-2H3
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| Chemical Name |
2-amino-7-(dimethylamino)-4-[3-(trifluoromethyl)phenyl]-4H-chromene-3-carbonitrile
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| Synonyms |
94G6; Chromeceptin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~278.3 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (27.83 mM) in 50% PEG300 +50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7828 mL | 13.9140 mL | 27.8280 mL | |
| 5 mM | 0.5566 mL | 2.7828 mL | 5.5656 mL | |
| 10 mM | 0.2783 mL | 1.3914 mL | 2.7828 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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