L-778123 HCl
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MedKoo CAT#: 206097

CAS#: 253863-00-2 (HCl)

Description: L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed.

Chemical Structure

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L-778123 HCl
CAS# 253863-00-2 (HCl)
Instruction

Theoretical Analysis

MedKoo Cat#: 206097
Name: L-778123 HCl
CAS#: 253863-00-2 (HCl)
Chemical Formula: C22H21Cl2N5O
Exact Mass: 0.00
Molecular Weight: 442.340
Elemental Analysis: C, 59.74; H, 4.79; Cl, 16.03; N, 15.83; O, 3.62

Price and Availability

Size Price Availability Quantity
10mg USD 110 Ready to ship
25mg USD 220 Ready to ship
50mg USD 400 Ready to ship
100mg USD 700 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 2650 Ready to ship
1g USD 4250 2 weeks
2g USD 7250 2 Weeks
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Related CAS #: 253863-00-2 (HCl)   183499-57-2 (free base)   183499-56-1 (2HCl)  

Synonym: L778123; L-778123; L 778123; L778,123; L-778,123; L 778,123 HCl; L-778123 hydrochloride

IUPAC/Chemical Name: 4-((5-((4-(3-chlorophenyl)-3-oxopiperazin-1-yl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile hydrochloride

InChi Key: YNBSQYGTJLIPJS-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H20ClN5O.ClH/c23-19-2-1-3-20(10-19)28-9-8-26(15-22(28)29)14-21-12-25-16-27(21)13-18-6-4-17(11-24)5-7-18;/h1-7,10,12,16H,8-9,13-15H2;1H

SMILES Code: N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 442.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Si MS, Reitz BA, Borie DC. Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123. Invest New Drugs. 2005 Jan;23(1):21-9. PubMed PMID: 15528977.

2: Martin NE, Brunner TB, Kiel KD, DeLaney TF, Regine WF, Mohiuddin M, Rosato EF, Haller DG, Stevenson JP, Smith D, Pramanik B, Tepper J, Tanaka WK, Morrison B, Deutsch P, Gupta AK, Muschel RJ, McKenna WG, Bernhard EJ, Hahn SM. A phase I trial of the dual farnesyltransferase and geranylgeranyltransferase inhibitor L-778,123 and radiotherapy for locally advanced pancreatic cancer. Clin Cancer Res. 2004 Aug 15;10(16):5447-54. PubMed PMID: 15328183.

3: Reid TS, Long SB, Beese LS. Crystallographic analysis reveals that anticancer clinical candidate L-778,123 inhibits protein farnesyltransferase and geranylgeranyltransferase-I by different binding modes. Biochemistry. 2004 Jul 20;43(28):9000-8. PubMed PMID: 15248757.

4: Huang XK, Meyer P, Li B, Raza A, Preisler HD. The effects of the farnesyl transferase inhibitor FTI L-778,123 on normal, myelodysplastic, and myeloid leukemia bone marrow progenitor proliferation in vitro. Leuk Lymphoma. 2003 Jan;44(1):157-64. PubMed PMID: 12691158.

5: Lobell RB, Liu D, Buser CA, Davide JP, DePuy E, Hamilton K, Koblan KS, Lee Y, Mosser S, Motzel SL, Abbruzzese JL, Fuchs CS, Rowinsky EK, Rubin EH, Sharma S, Deutsch PJ, Mazina KE, Morrison BW, Wildonger L, Yao SL, Kohl NE. 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):747-58. PubMed PMID: 12479371.

6: Hahn SM, Bernhard EJ, Regine W, Mohiuddin M, Haller DG, Stevenson JP, Smith D, Pramanik B, Tepper J, DeLaney TF, Kiel KD, Morrison B, Deutsch P, Muschel RJ, McKenna WG. A Phase I trial of the farnesyltransferase inhibitor L-778,123 and radiotherapy for locally advanced lung and head and neck cancer. Clin Cancer Res. 2002 May;8(5):1065-72. PubMed PMID: 12006520.

7: Britten CD, Rowinsky EK, Soignet S, Patnaik A, Yao SL, Deutsch P, Lee Y, Lobell RB, Mazina KE, McCreery H, Pezzuli S, Spriggs D. A phase I and pharmacological study of the farnesyl protein transferase inhibitor L-778,123 in patients with solid malignancies. Clin Cancer Res. 2001 Dec;7(12):3894-903. PubMed PMID: 11751480.

8: Buser CA, Dinsmore CJ, Fernandes C, Greenberg I, Hamilton K, Mosser SD, Walsh ES, Williams TM, Koblan KS. High-performance liquid chromatography/mass spectrometry characterization of Ki4B-Ras in PSN-1 cells treated with the prenyltransferase inhibitor L-778,123. Anal Biochem. 2001 Mar 1;290(1):126-37. PubMed PMID: 11180946.