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SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.
| Cell Experiment | |
|---|---|
| Cell lines | T-24, MCF-7, MCF-7/VP, NCI/ADR cell lines |
| Preparation method | T24, MCF-7, MCF-7/VP, and NCI/ADR cells are plated into 96-well tissue culture plates at ~15% confluency. 24 hours Later, treating the cells are with various concentrations of inhibitors. An additional 48 hours later , cell survival is assayed using the sulforhodamine B assay |
| Concentrations | ~50 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | JC xenografts are established in mice |
| Formulation | DMSO (ip), polyethylene glycol 400 (oral) |
| Dosages | ~100 mg/kg |
| Administration | Intraperitoneal administration or oral administration |
| 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.
| Molecular Weight | 302.78 |
| Formula | C15H11ClN2OS |
| CAS Number | 312636-16-1 |
| Purity | 99.36% |
| Solubility | DMSO 50 mg/mL |
| Storage | at -20°C |
| Related S1P Receptor Products |
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Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor, with IC50 of 1.88 nM in CHO cells. |
| PF-543 Citrate
PF-543 Citrate is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. |
| Opaganib (ABC294640)
Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. |
| NIBR-0213
NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist. |
| A-971432
A-971432 is an orally bioavailable, non-clastogenic, azetidinecarboxylate compound that acts as a highly potent and selective sphingosine-1-phosphate receptor 5 agonist (IC50 = 6 nM/S1P5, 362 nM/S1P1 and >10 μM/S1P3 in a radio-ligand binding assay). |
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