Methuosis inducer
- Product Name
- Methuosis inducer
- CAS No.
- 2240205-30-3
- Chemical Name
- Methuosis inducer
- Synonyms
- Methuosis inducer;Methuosis inducer 1;Methuosis inducer 1, 10 mM in DMSO;Inhibitor,Methuosis inducer 1,Methuosis inducer-1,inhibit,Methuosis inducer1;Benzamide, N-[4-methyl-3-[[6-(3-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]phenyl]-3-(trifluoromethyl)-
- CBNumber
- CB24819512
- Molecular Formula
- C27H20F3N5O
- Formula Weight
- 487.48
- MOL File
- 2240205-30-3.mol
Methuosis inducer Property
- Density
- 1.399±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 25 mg/mL (51.28 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C)
- form
- Solid
- pka
- 12.81±0.70(Predicted)
- color
- White to off-white
Methuosis inducer Chemical Properties,Usage,Production
Uses
HZX-02-059 is a potent methuosis inducer and dual-target PIKfyve/tubulin inhibitor with anticancer activity. Methuosis mainly disrupts the balance of endocytosis and exocytosis, forming a large number of vesicles and inducing cell death. HZX-02-059 also induces cell vacuolization, promotes apoptosis, downregulates the p53 pathway, inhibits PI3K/AKT phosphorylation, and inhibits c-Myc and NF-κB transcription[1][2].
Biological Activity
Methuosis inducer 1 is a potent methuosis inducer[1]. Anticancer activity[1]. Methuosis inducer 1 (Compound 13) shows a broad spectrum of cytotoxicity against a panel of human cancer cell lines with IC50 values of 0.326±0.026 μM, 1.370±0.061 μM, 1.662±0.128 μM, 1.892±0.092 μM, 1.571±0.066 μM, 2.268±0.100 μM, 2.611±0.739 μM, 1.008±0.042 μM, 1.566±0.015 μM, and 1.197±0.344 μM for A375, SK-MEL-28, SK-MEL-30, A549, MDA-MB-231, MDA-MB-435S, MCF-7, HCT116, BGC823, HepG2 cells, respectively[1].
References
[1]. Huang W, et al. Discovery and Identification of Small Molecules as Methuosis Inducers with in Vivo Antitumor Activities. J Med Chem. 2018 Jun 28;61(12):5424-5434.
Methuosis inducer Preparation Products And Raw materials
Raw materials
Preparation Products
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