ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM.
Adv Sci (Weinh). 2022 Jul;9(21):e2201414.
Bile Acid Conjugation on Solid Nanoparticles Enhances ASBT‐Mediated Endocytosis and Chylomicron Pathway but Weakens the Transcytosis by Inducing Transport
ZCL278 purchased from AbMole
Int J Pharm. 2022 Feb 14;617:121589.
Lipid raft-mediated and upregulated coordination pathways assist transport of glycocholic acid-modified nanoparticle in a human breast cancer cell line of SK-BR-3
ZCL278 purchased from AbMole
Int J Nanomedicine. 2018 Jul 27;13:4391-4404.
Rho GTPases in A549 and Caco-2 cells dominating the endocytic pathways of nanocarbons with different morphologies.
ZCL278 purchased from AbMole
ACS Appl Mater Interfaces. 2017 Feb 22;9(7):5803-5816.
Transmembrane Pathways and Mechanisms of Rod-like Paclitaxel Nanocrystals through MDCK Polarized Monolayer
ZCL278 purchased from AbMole
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Source | International Journal of Nanomedicine (2018). Figure 5. ZCL278 (Abmole Bioscience, Houston, TX, USA) |
| Method | RNA interference | |
| Cell Lines | A549 cells | |
| Concentrations | ||
| Incubation Time | 24 h | |
| Results | These findings indicated that Cdc42 played a vital role in the uptake of oxMWCNTs in A549 cells, while Rac1 and RhoA might not be involved in this process. |
. figure 9.jpg) |
Source | ACS Appl Mater Interfaces (2017). Figure 9. ZCL 278 (Abmole BioScience. Houston, TX, USA) |
| Method | Transwells | |
| Cell Lines | MDCK cells | |
| Concentrations | ||
| Incubation Time | ||
| Results | As shown in Figure 9, in the presence of ZCL 278, the transmembrane amount of PTX-NCs was reduced significantly, indicating that Cdc 42 participated in the regulation of the transport of PTX-NCs. |
| Molecular Weight | 584.89 |
| Formula | C21H19BrClN5O4S2 |
| CAS Number | 587841-73-4 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Natasha P Murphy, et al. Progress in the therapeutic inhibition of Cdc42 signalling
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