K858
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $980 | Check With Us |
| 500mg | $1550 | Check With Us |
| 1g | $2325 | Check With Us |
: Cat #: V2906 CAS #: 72926-24-0 Purity ≥ 98%
Description: K-858 is a novel, potent and ATP-uncompetitive inhibitor of mitotic kinesin Eg5 that has potential antitumor activity.
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- Physicochemical and Storage Information
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| Molecular Weight (MW) | 277.34 |
|---|---|
| Molecular Formula | C13H15N3O2S |
| CAS No. | 72926-24-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mM in DMSOr |
| Water: <1 mg/mLr | |
| Ethanol: | |
| SMILES Code | CC(NC1=NN(C(C)=O)C(C2=CC=CC=C2)(C)S1)=O |
| Synonyms | K-858; K 858; K858. |
| Protocol | In Vitro | K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM. K858 does not inhibit the ATPase activity of the mitotic kinesins CENP-E and MKLP1, or the conventional kinesin heavy chain even at 200 μM. K858 induces mitotic arrest and growth inhibition via the activation of the Mad2-mediated spindle checkpoint. K858 (5 μM) induces mitotic cell death in cancer cells but not in normal cells |
|---|---|---|
| In Vivo | K858 (50, 150 mg/kg, p.o.) shows antitumor activity in an A2780 ovarian cancer xenograft model, also inhibits tumor grwoth in a HCT116 colon cancer xenograft model via 100 mg/kg twice a day orally for 5 days. K858 (100 mg/kg, p.o., qd ×5) displays no neurotoxic side effects in mice |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.6057 mL | 18.0284 mL | 36.0568 mL | 72.1137 mL |
| 5mM | 0.7211 mL | 3.6057 mL | 7.2114 mL | 14.4227 mL |
| 10mM | 0.3606 mL | 1.8028 mL | 3.6057 mL | 7.2114 mL |
| 20mM | 0.1803 mL | 0.9014 mL | 1.8028 mL | 3.6057 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.