CP-609754 (OSI754, LNK 754)
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 |
|---|---|---|
| 100mg | $1550 | To Be Confirmed |
| 250mg | $2580 | To Be Confirmed |
| 500mg | $3870 | To Be Confirmed |
: Cat #: V3986 CAS #: 1190094-64-4 Purity ≥ 98%
Description: OSI754 (also known as CP-609754, CP-609,754, LNK-754) is a novel and potent farnesyltransferase inhibitor (TFI) that has potential anticancer activity.
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| Molecular Weight (MW) | 479.96 |
|---|---|
| Molecular Formula | C29H22ClN3O2 |
| CAS No. | 1190094-64-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 10 mMr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | O=C1N(C)C2=C(C=C([C@](O)(C3=CC=C(Cl)C=C3)C4=CN=CN4C)C=C2)C(C5=CC=CC(C#C)=C5)=C1 |
| Synonyms | CP-609754; CP609754; CP 609754; LNK 754; LNK754; LNK-754; OSI 754; OSI754; OSI-754 |
| Protocol | In Vitro | CP-609754 is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex and competes for the binding of the Ras protein. CP-609754 selectively inhibits farnesylation of both H- and K-Ras proteins in 3T3 transfectants. CP-609754 (CP-609,754) is a reversible inhibitor of farnesyltransferase with a slow on/off rate. CP-609,754 inhibits farnesylation (IC50=1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with SDS-PAGE analysis of [35S]methionine-labeled materia. |
|---|---|---|
| In Vivo | With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, and tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL. With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED50 for tumor growth inhibition is 28 mg/kg. CP-609754 (CP-609,754) has antitumor activity against 3T3 H-ras (61L) tumors in vivo. |
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 | 2.0835 mL | 10.4175 mL | 20.8351 mL | 41.6701 mL |
| 5mM | 0.4167 mL | 2.0835 mL | 4.1670 mL | 8.3340 mL |
| 10mM | 0.2084 mL | 1.0418 mL | 2.0835 mL | 4.1670 mL |
| 20mM | 0.1042 mL | 0.5209 mL | 1.0418 mL | 2.0835 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
mg
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,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.