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Chemical Structure| 1208222-39-2 Chemical Structure| 1208222-39-2

Structure of VU 0365114
CAS No.: 1208222-39-2

Chemical Structure| 1208222-39-2

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VU 0365114 is a allosteric modulator of M5 with EC50 of 2.7 μM.

4.5 *For Research Use Only !

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Product Details of VU 0365114

CAS No. :1208222-39-2
Formula : C22H14F3NO3
M.W : 397.35
SMILES Code : O=C1N(CC2=CC=C(C3=CC=CC=C3)C=C2)C4=C(C=C(OC(F)(F)F)C=C4)C1=O
MDL No. :MFCD22683818
InChI Key :SPBGRXOPAXZSER-UHFFFAOYSA-N
Pubchem ID :45281794

Safety of VU 0365114

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
AsPC-1 and PANC-1 cells 10 µM 18 hours RNA sequencing analysis of VU-0365114's gene expression profiles showed high similarity to microtubule-destabilizing agents. Mol Oncol. 2024 Feb;18(2):386-414
HeLa cells 10 µM 24 hours To examine the effect of VU-0365114 on apoptosis, results showed induction of PARP and caspase-3 cleavage. Mol Oncol. 2024 Feb;18(2):386-414
HeLa cells 10 µM 24 hours To examine the effect of VU-0365114 on the cell cycle, results showed induction of G2/M cell-cycle arrest. Mol Oncol. 2024 Feb;18(2):386-414
HeLa cells 10 µM 3 hours To examine the effect of VU-0365114 on microtubule assembly, results showed that VU-0365114 reduced the polymerized fractions of microtubules. Mol Oncol. 2024 Feb;18(2):386-414
HeLa-Kyoto-tubulin-EGFP/H2B-mCherry cells 10 µM 4 hours To observe the effect of VU-0365114 on microtubule organization, results showed microtubule fragments scattered in the cytoplasm. Mol Oncol. 2024 Feb;18(2):386-414
MES-SA and MES-SA/Dx5 cells 10 µM 72 hours To examine the effect of VU-0365114 on multidrug-resistant cells, results showed that VU-0365114 could overcome MDR. Mol Oncol. 2024 Feb;18(2):386-414

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/C nude mice HCT116 tumor xenograft model Intraperitoneal injection 5 mg/kg Once daily for 5 days To evaluate the effect of VU-0365114 on in vivo colorectal tumor growth, results showed that VU-0365114 slowed the growth of HCT116 xenograft. Mol Oncol. 2024 Feb;18(2):386-414

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.17mL

5.03mL

2.52mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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