L-778123 hydrochloride

Name: L-778123 hydrochloride
Brand: MedChemExpress
SKU: HY-16273A
Rating: 4.5 (1 reviews)

Cat. No.: HY-16273A Purity: 98.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC₅₀ values of 2 nM and 98 nM respectively.

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

L-778123 hydrochloride Chemical Structure

CAS No. : 253863-00-2

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 85	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 85	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 319	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 539	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of L-778123 hydrochloride:

L-778123 Get quote

1 Publications Citing Use of MCE L-778123 hydrochloride

•bioRxiv. 2023 Feb 8:2023.02.07.527548. [Abstract]

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Biological Activity
Purity & Documentation
References
Customer Review

Description

L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC₅₀ values of 2 nM and 98 nM respectively.

In Vitro

L-778123 hydrochloride 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 hydrochloride 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) hydrochloride 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) hydrochloride 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.

In Vivo

L-778123 (50 mg/kg/day, infusion, 7 days) hydrochloride 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.

Clinical Trial

Molecular Weight

442.34

Formula

C₂₂H₂₁Cl₂N₅O

CAS No.

253863-00-2

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.[H]Cl

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

In Vitro:

DMSO : ≥ 25 mg/mL (56.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (56.52 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
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

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: ≥ 2.25 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: ≥ 2.25 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.25 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (226.07 mM); Suspended solution; Need ultrasonic and adjust pH to 5 with 1M HCl

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 98.96%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (257 KB) HNMR (262 KB) LCMS (108 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. Fredrick O. Onono, et al. The Farnesyltransferase Inhibitor (FTI) L-778,123 Displays Promising Anti-Leukemia Activity. Blood (2008); 112 (11): 2627.

[4]. Si MS, et al. Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123. Invest New Drugs. 2005 Jan;23(1):21-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.2607 mL	11.3035 mL	22.6070 mL	56.5176 mL
	5 mM	0.4521 mL	2.2607 mL	4.5214 mL	11.3035 mL
	10 mM	0.2261 mL	1.1304 mL	2.2607 mL	5.6518 mL
	15 mM	0.1507 mL	0.7536 mL	1.5071 mL	3.7678 mL
	20 mM	0.1130 mL	0.5652 mL	1.1304 mL	2.8259 mL
	25 mM	0.0904 mL	0.4521 mL	0.9043 mL	2.2607 mL
	30 mM	0.0754 mL	0.3768 mL	0.7536 mL	1.8839 mL
	40 mM	0.0565 mL	0.2826 mL	0.5652 mL	1.4129 mL
	50 mM	0.0452 mL	0.2261 mL	0.4521 mL	1.1304 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.