HEMTAC WEE1 degrader-1

Name: HEMTAC WEE1 degrader-1
Brand: MedChemExpress
SKU: HY-173320
Rating: 4.5 (1 reviews)

Cat. No.: HY-173320 Purity: 99.78%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC₅₀: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker).

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

HEMTAC WEE1 degrader-1 Chemical Structure

CAS No. : 3002417-64-0

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

IC₅₀ & Target

HSP90

16.76 nM (IC₅₀)

Hsp90TACs

In Vitro

HEMTAC WEE1 degrader-1 (Compound 9c) (72 h) inhibits the proliferation activity of MV-4-11 cells (IC₅₀: 8.08 nM) and primary AML cells (IC₅₀: 4.77 nM)^[1].
HEMTAC WEE1 degrader-1 (0.01-10 μM, 12 h) degrades WEE1 protein in MV-4-11 cells and has a minor effect on AKT protein, indicating that this effect is independent of HSP90 inhibition^[1].
HEMTAC WEE1 degrader-1 (0.1-10 μM, 12 h) promotes the expression of WEE1 mRNA in MV-4-11 cells in a concentration-dependent manner^[1].
HEMTAC WEE1 degrader-1 (3-30 nM, 72 h) induces cell cycle arrest at the G2/M phase of MV-4-11 cells in a concentration-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:	MV-4-11 cells
Concentration:	0.01 μM, 0.1 μM, 1 μM and 10 μM
Incubation Time:	12 h
Result:	Down-regulated the expression of WEE1 protein.

RT-PCR^[1]

Cell Line:	MV-4-11 cells
Concentration:	0.1 μM, 1 μM and 10 μM
Incubation Time:	12 h
Result:	Up-regulated the expression of WEE1 mRNA.

Cell Cycle Analysis^[1]

Cell Line:	MV-4-11 cells
Concentration:	3 nM, 10 nM and 30 nM
Incubation Time:	72 h
Result:	Induced a large accumulation of cells in the G2/M phase.

In Vivo

HEMTAC WEE1 degrader-1 (Compound 9c) (3 mg/kg, i.v., once every day for 4 weeks) has anticancer activity with minimal toxicity in a mouse AML patient-derived xenograft (PDX) model^[1].
HEMTAC WEE1 degrader-1 (10 mg/kg, i.v., once every day for 3 d) has minimal myelosuppressive toxicity in healthy mice^[1].

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

Animal Model:	AML patient-derived xenograft (PDX) model, Female NOD/SCID mice (6-9 weeks old)^[1]
Dosage:	3 mg/kg
Administration:	Intravenous injection (i.v.), once every day for 4 weeks
Result:	Reduced the percentage of huCD45-positive cells in the bone marrow (>75%). Inhibited splenomegaly.

Animal Model:	Healthy male BALA/C mice (20-22 g)^[1]
Dosage:	10 mg/kg
Administration:	Intravenous injection (i.v.), once every day for 3 d
Result:	Had minimal effect on platelets, leukocytes and neutrophils

Molecular Weight

1062.27

Formula

C₅₇H₇₁N₁₅O₆

CAS No.

3002417-64-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NN=C(C2=CC(C(C)C)=C(O)C=C2O)N1C3=CC=C(CN4CCN(CC(NCCCCN5CCN(C6=CC=C(NC7=NC=C8C(N(C9=NC(C(C)(O)C)=CC=C9)N(CC=C)C8=O)=N7)C=C6)CC5)=O)CC4)C=C3)NCC

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 (94.14 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	0.9414 mL	4.7069 mL	9.4138 mL
5 mM	0.1883 mL	0.9414 mL	1.8828 mL
10 mM	0.0941 mL	0.4707 mL	0.9414 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 (2.35 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.35 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: 99.78%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (245 KB) HNMR (151 KB) RP-HPLC (168 KB) LCMS (236 KB)

Handling Instructions (2659 KB)

References

[1]. Li X, et al. Design, synthesis and biological evaluation of WEE1 degraders via HSP90-mediated targeting chimeras for target therapy of acute myeloid leukemia. Eur J Med Chem. 2025 Jun 5;290:117512. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	0.9414 mL	4.7069 mL	9.4138 mL	23.5345 mL
	5 mM	0.1883 mL	0.9414 mL	1.8828 mL	4.7069 mL
	10 mM	0.0941 mL	0.4707 mL	0.9414 mL	2.3535 mL
	15 mM	0.0628 mL	0.3138 mL	0.6276 mL	1.5690 mL
	20 mM	0.0471 mL	0.2353 mL	0.4707 mL	1.1767 mL
	25 mM	0.0377 mL	0.1883 mL	0.3766 mL	0.9414 mL
	30 mM	0.0314 mL	0.1569 mL	0.3138 mL	0.7845 mL
	40 mM	0.0235 mL	0.1177 mL	0.2353 mL	0.5884 mL
	50 mM	0.0188 mL	0.0941 mL	0.1883 mL	0.4707 mL
	60 mM	0.0157 mL	0.0784 mL	0.1569 mL	0.3922 mL
	80 mM	0.0118 mL	0.0588 mL	0.1177 mL	0.2942 mL