2. Membrane Transporter/Ion Channel Apoptosis
  3. CRM1 Apoptosis
  4. Felezonexor

Felezonexor  (Synonyms: CBS9106; SL-801)

Cat. No.: HY-108716 Purity: 98.84%
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CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells.

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

Felezonexor Chemical Structure

Felezonexor Chemical Structure

CAS No. : 1076235-04-5

Size Price Stock Quantity
1 mg USD 320 In-stock
5 mg USD 780 In-stock
10 mg USD 1100 In-stock
25 mg USD 1700 In-stock
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Based on 1 publication(s) in Google Scholar

Felezonexor Related Antibodies

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Description

CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells[1].

IC50 & Target

CRM1[1]
In Vitro

CBS9106 (0.01-10 μM; 72 hours) sensitizes cells to radiation and to suppress the growth of a variety of cancer cell lines. The estimated IC50 values range from 22.3 or 35.6 nM in multiple myeloma (MM).1S or RPMI-8226 cells and from 3 to 278 nM in 60 other human cancer cell lines[1].
CBS9106 (1-400 nM; 24 hours) decreases CRM1 protein expression levels in a dose-dependent manner[1].

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

Felezonexor Related Antibodies

Cell Viability Assay[1]

Cell Line: MM.1S cells, RPMI-8226 cells
Concentration: 0.01, 0.1, 10 μM
Incubation Time: 72 hours
Result: Suppressed the growth of a variety of cancer cell lines and the estimated IC50 values ranged from 22.3 or 35.6 nM in MM.1S or RPMI-8226 cells.

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 1, 3, 6, 12, 25, 50, 100, 200, 400 nM
Incubation Time: 24 hours
Result: The level of CRM1 protein expression markedly reduced in a dose-dependent manner.
In Vivo

CBS9106 (31.25-62.5 mg/kg for 5 times weekly, 125 mg/kg for 3 times weekly; p.o.; 2 weeks) significantly suppresses tumor growth at dose levels of 62.5 or 125 mg/kg in mice bearing human MM xenograft models[1].

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

Animal Model: SCID mice with RPMI-8226 cells[1]
Dosage: 31.25, 62.5, 125 mg/kg
Administration: Oal administration; 5 times weekly (31.25 and 62.5 mg/kg), 3 times weekly (125 mg/kg); 2 weeks
Result: Showed statistically significant tumor growth inhibition at dose levels of 62.5 mg/kg or 125 mg/kg.
Molecular Weight

419.83

Formula

C18H21ClF3N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(COCCC(C)(C)C)=C1C)N(NC2=NC(Cl)=C(C(F)(F)F)C=C2)C1=O
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 (238.19 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 2.3819 mL 11.9096 mL 23.8192 mL
5 mM 0.4764 mL 2.3819 mL 4.7638 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.

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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: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2.3819 mL 11.9096 mL 23.8192 mL 59.5479 mL
5 mM 0.4764 mL 2.3819 mL 4.7638 mL 11.9096 mL
10 mM 0.2382 mL 1.1910 mL 2.3819 mL 5.9548 mL
15 mM 0.1588 mL 0.7940 mL 1.5879 mL 3.9699 mL
20 mM 0.1191 mL 0.5955 mL 1.1910 mL 2.9774 mL
25 mM 0.0953 mL 0.4764 mL 0.9528 mL 2.3819 mL
30 mM 0.0794 mL 0.3970 mL 0.7940 mL 1.9849 mL
40 mM 0.0595 mL 0.2977 mL 0.5955 mL 1.4887 mL
50 mM 0.0476 mL 0.2382 mL 0.4764 mL 1.1910 mL
60 mM 0.0397 mL 0.1985 mL 0.3970 mL 0.9925 mL
80 mM 0.0298 mL 0.1489 mL 0.2977 mL 0.7443 mL
100 mM 0.0238 mL 0.1191 mL 0.2382 mL 0.5955 mL
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Felezonexor 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:

Felezonexor1076235-04-5CBS9106 SL-801CBS 9106CBS-9106SL801SL 801SL-801CRM1ApoptosisChromosomal Maintenance 1Exportin 1XPO1Inhibitorinhibitorinhibit

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