2. Metabolic Enzyme/Protease
  3. Farnesyl Transferase
  4. L-778123

L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively.

For research use only. We do not sell to patients.

L-778123 Chemical Structure

L-778123 Chemical Structure

CAS No. : 183499-57-2

Size Price Stock Quantity
5 mg USD 77 In-stock
10 mg USD 110 In-stock
25 mg USD 200 In-stock
50 mg USD 319 In-stock
100 mg USD 539 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of L-778123:

L-778123 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively[1][2].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1.72 μM
Compound: 51; L-788,123
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
[PMID: 33228976]
A549 IC50
100.72 μM
Compound: 51; L-788,123
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay
[PMID: 33228976]
HT-29 IC50
1.52 μM
Compound: 51; L-788,123
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay
[PMID: 33228976]
HT-29 IC50
125.78 μM
Compound: 51; L-788,123
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay
[PMID: 33228976]
In Vitro

L-778123 alone does not have obvious cytotoxicity on HT-29 and A549 cell lines (IC50: >100 μM), but can generate synergistic effects with Doxorubicin (HY-15142A), with the decreased IC50s of 1.72 and 1.52 μM respectively[2].
L-778123 inhibits myeloid leukemia cell proliferation with IC50 values of 0.2 μM-1.8 μM for cell lines, and 0.1 μM-161.8 μM in primary samples[3].
L-778123 (0-1 μM, 12 h; or 5 μM, 6 h) inhibits H-RAS prenylation in HL-60 cells, and inhibits phosphorylated MEK-1/2 level (5 μM, 24 h)[3].
L-778123 (0-100 μM, 72 h) inhibits lymphocyte activation (marker: CD71 or CD25) and function in human PBMCs[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

L-778123 Related Antibodies
In Vivo

L-778123 (50 mg/kg/day, infusion, 7 days) inhibits both HDJ2 and Rap1A prenylation in PBMCs of dogs, but without inhibition in Ki-Ras prenylation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

405.88

Formula

C22H20ClN5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (49.28 mM; ultrasonic and adjust pH to 2 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4638 mL 12.3189 mL 24.6378 mL
5 mM 0.4928 mL 2.4638 mL 4.9276 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (4.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (4.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4638 mL 12.3189 mL 24.6378 mL 61.5946 mL
5 mM 0.4928 mL 2.4638 mL 4.9276 mL 12.3189 mL
10 mM 0.2464 mL 1.2319 mL 2.4638 mL 6.1595 mL
15 mM 0.1643 mL 0.8213 mL 1.6425 mL 4.1063 mL
20 mM 0.1232 mL 0.6159 mL 1.2319 mL 3.0797 mL
25 mM 0.0986 mL 0.4928 mL 0.9855 mL 2.4638 mL
30 mM 0.0821 mL 0.4106 mL 0.8213 mL 2.0532 mL
40 mM 0.0616 mL 0.3080 mL 0.6159 mL 1.5399 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

L-778123 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-778123183499-57-2L778123L 778123Farnesyl TransferaseFtaseAnti-LeukemiaprenylationHL-60 cellInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
L-778123
Cat. No.:
HY-16273
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.