PROTAC XPO1 degrader-1

Name: PROTAC XPO1 degrader-1
Brand: MedChemExpress
SKU: HY-170669
Rating: 4.5 (1 reviews)

Cat. No.: HY-170669 Purity: 99.77%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)).

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

PROTAC XPO1 degrader-1 Chemical Structure

CAS No. : 3105680-00-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

PROTAC XPO1 degrader-1 (Compound 2c) effectively degrades XPO1 protein in MV4-11 acute myeloid leukemia (AML) cells with a DC₅₀ of 23.67 nM^[1].

PROTAC XPO1 degrader-1 exhibits significant anti-proliferative effects, with IC₅₀ values of 0.142 μM and 0.186 μM against MV4-11 and MOLM-13 cells, respectively^[1].

PROTAC XPO1 degrader-1 (100-500 nM; 24 h) effectively induces apoptosis in MV4-11 cells through the caspase pathway^[1].

PROTAC XPO1 degrader-1 (100-200 nM; 24 h) can arrest the cell cycle of MV4-11 cells in the G1 phase^[1].

PROTAC XPO1 degrader-1 (50 nM; 24 h) reduces cell migration in MV4-11 cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:	MV4-11
Concentration:	100, 200, 500 nM
Incubation Time:	24 h
Result:	Induced apoptosis in 71.4 % of the cells at a concentration of 200 nM. Significantly increased the activation of caspase-3/7 in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:	MV4-11
Concentration:	5, 10, 25, 50, 100 ,500 nM
Incubation Time:	12 h
Result:	Reduced the protein level of XPO1 in cells in a concentration-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:	MV4-11
Concentration:	100, 200 nM
Incubation Time:	24 h
Result:	Caused the proportion of cells arrested in the G1 phase to rise from 39.50% to 60.28% as the concentration increased (from 0 to 200 nM).

Cell Migration Assay ^[1]

Cell Line:	MV4-11
Concentration:	50 nM
Incubation Time:	24 h
Result:	Resulted in approximately a 42.6 % reduction in MV4-11 cell migration at 50 nM.

Molecular Weight

734.12

Formula

C₃₃H₃₅ClF₃N₇O₇

CAS No.

3105680-00-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC1=C(C(F)(F)F)C=CC(NN2C(C(C)=C(CCC(NCC3CCN(C4=CC=C(C(NC5C(NC(CC5)=O)=O)=O)C(OC)=C4)CC3)=O)C2=O)=O)=N1

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 (136.22 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	1.3622 mL	6.8109 mL	13.6218 mL
5 mM	0.2724 mL	1.3622 mL	2.7244 mL
10 mM	0.1362 mL	0.6811 mL	1.3622 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (3.41 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 (3.41 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

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

Purity: 99.77%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (245 KB) HNMR (152 KB) RP-HPLC (169 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Chen G, et al. Discovery of novel XPO1 PROTAC degraders for the treatment of acute myeloid leukemia[J]. European Journal of Medicinal Chemistry, 2025, 283: 117182. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.3622 mL	6.8109 mL	13.6218 mL	34.0544 mL
	5 mM	0.2724 mL	1.3622 mL	2.7244 mL	6.8109 mL
	10 mM	0.1362 mL	0.6811 mL	1.3622 mL	3.4054 mL
	15 mM	0.0908 mL	0.4541 mL	0.9081 mL	2.2703 mL
	20 mM	0.0681 mL	0.3405 mL	0.6811 mL	1.7027 mL
	25 mM	0.0545 mL	0.2724 mL	0.5449 mL	1.3622 mL
	30 mM	0.0454 mL	0.2270 mL	0.4541 mL	1.1351 mL
	40 mM	0.0341 mL	0.1703 mL	0.3405 mL	0.8514 mL
	50 mM	0.0272 mL	0.1362 mL	0.2724 mL	0.6811 mL
	60 mM	0.0227 mL	0.1135 mL	0.2270 mL	0.5676 mL
	80 mM	0.0170 mL	0.0851 mL	0.1703 mL	0.4257 mL
	100 mM	0.0136 mL	0.0681 mL	0.1362 mL	0.3405 mL