[CAS NO. 253863-00-2] L-778123hydrochloride
PRODUCTS SPECIFICATIONS [253863-00-2]
DESCRIPTION [253863-00-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 442.34 |
| Molecular Formula | C22H21Cl2N5O |
| SMILES | N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl |
Summary
L-778123 hydrochloride is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination. IC50 value: 2 nM [1] Target: FPTase in vitro: L-778123 can completely inhibit Ki-Ras prenylation. [1] L-778123 as a farnesyltransferase inhibitor can have a good cytotoxic activity as a classic anti-cancer agent. [2] in vivo: In the dog model, L-778123 inhibits HDJ2 prenylation and produces measurable, albeit slight (5%), levels of unprenylated Rap1A in PBMCs. [1]
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00004057 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific
|
December 1998 | Phase 1 |
| NCT00003430 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Head and Neck Cancer|Unspecified Adult Solid Tumor, Protocol Specific
|
April 1998 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 25 mg/mL ( 56.52 mM )
H 2 O : 25 mg/mL ( 56.52 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2607 mL | 11.3035 mL | 22.6070 mL |
| 5 mM | 0.4521 mL | 2.2607 mL | 4.5214 mL |
| 10 mM | 0.2261 mL | 1.1304 mL | 2.2607 mL |
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1.
Add each solvent one by one: PBS
Solubility: 20 mg/mL (45.21 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.25 mg/mL (5.09 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.25 mg/mL (5.09 mM); Clear solution
References
- [1] Lobell RB, et al. Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther. 2002 Jul;1(9):747-758.
- [2] Ghasemi S, et al. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines. Adv Pharm Bull. 2013;3(1):73-77.
Synonyms
