Vimentin-IN-1 - ≥99% , CAS No.2319587-80-7

CAS: 2319587-80-7 Cat. No.: V651394 Molecular Weight: 389.28

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin ( VIM ), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1

In Vitro

Vimentin-IN-1 (compound 4e) (0-10 mM; 72 h) inhibits a marked improvement in potency with an IC 50 value of 44 nM against HT-1080 fibrosarcoma, better than than FiVe1 (IC 50 =1.6 μM, HT-1080). Vimentin-IN-1 (0.1 μM; 24 h) induces phosphorylation of VIM at Ser56. Vimentin-IN-1 (100 μM; sampled at 0, 5, 15, 30, 45, and 60 min) exhibits poor stability with 0.0% remaining after 60 min of incubation in mouse liver microsome. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HT-1080, RD, and MCF-7 cells Concentration: 0-10 mM Incubation Time: 72 hours Result: Inhibited HT-1080, RD, and MCF-7 cells with IC 50 s of 44 nM, 61 nM, and 49 nM, respectively.

In Vivo

Vimentin-IN-1 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1 . Pharmacokinetic properties of Vimentin-IN-1 in mice Route Dose (mg/kg) AUC 0-last (ng·h/mL) AUC 0-inf (ng·h/mL) T 1/2 (h) T max (h) T last (h) C max (ng/mL) 4e PO 10 371.33 534.33 4.68 0.67 8 154.67 4e IP 1 208.33 211.33 0.59 0.25 4 197.00 Five1 PO 25 309.78 339.21 4.57 0.5 18 110.43 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:vimentin (VIM)

Specifications

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type IIIxa0intermediate filament protein vimentin ( VIM ), to induce hyperphosphorylationxa0of Ser56, resulting selective disruption of mitosis and multinucl

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Purity

≥99%

Names and Identifiers

• Canonical Smiles: COC1=CC(Cl)=CC(N2CCN(C3=C4C=CC=C(Cl)C4=NN=C3)CC2)=C1
• Molecular Weight: 389.28

Chemical and Physical Properties

• Solubility: DMSO : 25 mg/mL (64.22 mM; Need ultrasonic)

References

1. Hong-Qin Wang, Bu-Yun Yu, Zi-Yang Huang, Fang-Zhou Wang, Lu Ju, Zhi-Da Xiao, Jun-Lin Zhan, Hao Chen, Zhen-Guo Liu, Wei-Bing Lu, Cheng-Hui Li.  (2024)  Shape-adaptive and recyclable radio-frequency devices based on polymer with variable stiffness.  Cell Reports Physical Science,      [PMID:] [10.1016/j.xcrp.2024.101882]