1. Apoptosis
  2. Bcl-2 Family
  3. FCN-338

FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC50 of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL.

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FCN-338

FCN-338 Chemical Structure

CAS No. : 2248046-39-9

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Based on 1 publication(s) in Google Scholar

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Description

FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC50 of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL[1][2].

IC50 & Targetinhibitor

BCL2

 

Clinical Trial
Molecular Weight

902.46

Formula

C48H48ClN7O7S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC=C(C=C1)C(CC(C)(CC2)C)=C2CN3CCN(C4=CC=C(C(NS(=O)(C5=CC(OC6)=C(C([N+]([O-])=O)=C5)N[C@H]6CC7=CC=CC=C7)=O)=O)C(OC8=CN=C9NC=CC9=C8)=C4)CC3

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 : 100 mg/mL (110.81 mM; Need ultrasonic; 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 1.1081 mL 5.5404 mL 11.0808 mL
5 mM 0.2216 mL 1.1081 mL 2.2162 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)

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Concentration
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Volume
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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

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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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (5.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 1.1081 mL 5.5404 mL 11.0808 mL 27.7021 mL
5 mM 0.2216 mL 1.1081 mL 2.2162 mL 5.5404 mL
10 mM 0.1108 mL 0.5540 mL 1.1081 mL 2.7702 mL
15 mM 0.0739 mL 0.3694 mL 0.7387 mL 1.8468 mL
20 mM 0.0554 mL 0.2770 mL 0.5540 mL 1.3851 mL
25 mM 0.0443 mL 0.2216 mL 0.4432 mL 1.1081 mL
30 mM 0.0369 mL 0.1847 mL 0.3694 mL 0.9234 mL
40 mM 0.0277 mL 0.1385 mL 0.2770 mL 0.6926 mL
50 mM 0.0222 mL 0.1108 mL 0.2216 mL 0.5540 mL
60 mM 0.0185 mL 0.0923 mL 0.1847 mL 0.4617 mL
80 mM 0.0139 mL 0.0693 mL 0.1385 mL 0.3463 mL
100 mM 0.0111 mL 0.0554 mL 0.1108 mL 0.2770 mL
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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.

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Product Name:
FCN-338
Cat. No.:
HY-175342
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