Cat. No.: HY-170669

PROTAC XPO1 degrader-1

Name: PROTAC XPO1 degrader-1
Brand: MedChemExpress
SKU: HY-170669
Price: 480.00 USD
Availability: InStock
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PROTAC XPO1 degrader-1 is a CRBN-recruiting PROTAC degrader of exportin 1 (XPO1), with a DC₅₀ of 23.67 nM. It exerts anti-proliferative effects against acute myeloid leukemia cells by inducing XPO1 protein degradation, inhibiting NF-κB activity, inducing apoptosis, and causing G1 cell cycle arrest. PROTAC XPO1 degrader-1 can be used for research on acute myeloid leukemia.
(Pink: CRM1 ligand (HY-170672); Blue: Cereblon ligand (HY-170671); Black: linker (HY-W010525)).

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

Purity : 99.77%
CAS No.: 3105680-00-7
Formula: C₃₃H₃₅ClF₃N₇O₇
Molecular Weight:734.12

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PROTAC XPO1 degrader-1 Chemical Structure

CAS No.: 3105680-00-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

HY-D0843
N-Ethylmaleimide

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC XPO1 degrader-1 is a CRBN-recruiting PROTAC degrader of exportin 1 (XPO1), with a DC₅₀ of 23.67 nM. It exerts anti-proliferative effects against acute myeloid leukemia cells by inducing XPO1 protein degradation, inhibiting NF-κB activity, inducing apoptosis, and causing G1 cell cycle arrest. PROTAC XPO1 degrader-1 can be used for research on acute myeloid leukemia^[1]. (Pink: CRM1 ligand (HY-170672); Blue: Cereblon ligand (HY-170671); Black: linker (HY-W010525)).

IC₅₀ & Target

^[1]

XPO1

23.67 nM (DC₅₀)

All PROTACs Isoforms :

All NF-κB Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	0.142 μM	Antiproliferative activity against human acute monocytic leukemia MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human acute monocytic leukemia MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.	39708768
MOLM-13	IC₅₀	0.186 μM	Antiproliferative activity against human acute monocytic leukemia MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay. Antiproliferative activity against human acute monocytic leukemia MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.	39708768
MV4-11	DC₅₀	23.67 nM	Degradation of XPO1 protein in human acute monocytic leukemia MV4-11 cells measured by western blot assay with 12 hrs incubation. Degradation of XPO1 protein in human acute monocytic leukemia MV4-11 cells measured by western blot assay with 12 hrs incubation.	39708768

In Vitro

PROTAC XPO1 degrader-1 (compound 2c) (72 h) potently inhibits the proliferation of MV4-11 cells with an IC₅₀ of 0.142 μM; it also inhibits the proliferation of MOLM-13 cells with an IC₅₀ of 0.186 μM^[1].
PROTAC XPO1 degrader-1 (5-500 nM; 12 h) induces concentration-dependent degradation of XPO1 in MV4-11 cells, with a DC₅₀ of 23.67 nM; near-complete degradation is achieved within 12 h at a concentration of 100 nM, without altering the mRNA level of XPO1^[1].
PROTAC XPO1 degrader-1 (100 nM; 12 h) mediates the degradation of XPO1 in MV4-11 cells via the CRBN-dependent proteasomal pathway^[1].
PROTAC XPO1 degrader-1 (200 nM; 24 h) induces apoptosis in 71.4% of MV4-11 cells^[1].
PROTAC XPO1 degrader-1 (100-500 nM; 24 h) induces concentration-dependent activation of caspase-3/7 in MV4-11 cells^[1].
PROTAC XPO1 degrader-1 (100-200 nM; 24 h) induces concentration-dependent G1 phase arrest in MV4-11 cells, increasing the proportion of G1 phase cells to 60.28%^[1].
PROTAC XPO1 degrader-1 (200 nM; 24 h) inhibits TNF-α-induced NF-κB activation by 72% in MV4-11 cells^[1].
PROTAC XPO1 degrader-1 (50 nM; 24 h) reduces the migration rate of MV4-11 cells by 42.6%^[1].

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

Western Blot Analysis^[1]

Cell Line:

human acute monocytic leukemia MV4-11 cells
Concentration:

5, 10, 25, 50, 100, 500 nM (concentration-dependent degradation assay); 100 nM (time-course degradation assay)
Incubation Time:

12 h (concentration-dependent degradation assay); 4, 8, 16, 24, 36, 48 h (time-course degradation assay)
Result:

Induced concentration-dependent degradation of XPO1 with a DC₅₀ of 23.67 nM.
Achieved near-complete degradation of XPO1 at 100 nM after 12 h incubation.
Induced over 50% XPO1 degradation within 8 h at 100 nM.
Showed nearly complete XPO1 degradation after 16 h at 100 nM.
Caused XPO1 protein levels to begin recovering after 24 h while remaining significantly degraded.
Did not affect XPO1 mRNA levels.

Apoptosis Analysis^[1]

Cell Line:

human acute monocytic leukemia MV4-11 cells
Concentration:

100, 200 nM
Incubation Time:

24 h
Result:

Induced apoptosis in 71.4% of MV4-11 cells at 200 nM.

Cell Cycle Analysis^[1]

Cell Line:

human acute monocytic leukemia MV4-11 cells
Concentration:

100, 200 nM
Incubation Time:

24 h
Result:

Induced concentration-dependent G1 phase arrest.
Increased the percentage of cells in G1 phase from 39.50% to 60.28% at 200 nM.

ELISA Assay^[1]

Cell Line:

human acute monocytic leukemia MV4-11 cells
Concentration:

200 nM
Incubation Time:

24 h
Result:

Inhibited TNF-α-induced NF-κB activation by 72% at 200 nM.

Cell Migration Assay ^[1]

Cell Line:

human acute monocytic leukemia MV4-11 cells
Concentration:

50 nM
Incubation Time:

24 h
Result:

Reduced MV4-11 cell migration by approximately 42.6% relative to the control group.

Western Blot Analysis^[1]

Cell Line:

human acute monocytic leukemia MV4-11 cells
Concentration:

100 nM
Incubation Time:

12 h
Result:

Pretreatment with MG132, MLN4924, or thalidomide completely blocked XPO1 degradation induced by the reagent.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	F
Rat^[1]	1 mg/kg	i.v.	3.04 h	0.083 h	95.1 ng/mL	82.6 ng/mL·h	100 ng/mL·h	2.12 h	3.89 h	/
Rat^[1]	10 mg/kg	p.o.	3.98 h	1.5 h	24.4 ng/mL	82.6 ng/mL·h	95.1 ng/mL·h	2.75 h	4.75 h	9.51 %

In Vivo

PROTAC XPO1 degrader-1 (compound 2c (1.0-10 mg/kg; intravenous injection, oral administration; single dose)) exhibits desirable half-lives via both intravenous and oral routes in healthy male Sprague-Dawley rats, but shows low oral bioavailability of only 9.51%^[1].

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

Chemical Information

CAS No. 3105680-00-7
Appearance Solid
Molecular Weight 734.12
Formula C₃₃H₃₅ClF₃N₇O₇
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Chen G, et al. Discovery of novel XPO1 PROTAC degraders for the treatment of acute myeloid leukemia. European journal of medicinal chemistry. 2025 Feb 05;283:117182. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.3622 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

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PROTAC XPO1 degrader-1

All PROTACs Isoforms

All NF-κB Isoforms