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Cat. No.: HY-175810

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GSPT1 degrader-8

GSPT1 degrader-8 is a potent and orally active G1 to S phase transition 1 (GSPT1) molecular glue degrader. GSPT1 degrader-8 induces GSPT1 degradation and inhibits tumor growth. GSPT1 degrader-8 can be used for the research of cancer, such as breast cancer.

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

Formula: C₂₇H₂₃N₃O₄
Molecular Weight:453.49

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

GSPT1 degrader-8 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

In Vitro

GSPT1 degrader-8 (Compound 26) shows inhibitory activity against HCC1569 and N87 cells with IC₅₀ values of 0.19 nM and 0.29 nM^[1].
GSPT1 degrader-8 (3.3-300 nM, 24 h) induces degradation of GSPT1 in N87 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

N87 cells
Concentration:

3.3, 11, 33, 100 and 300 nM
Incubation Time:

24 h
Result:

Induced degradation of GSPT1

Parmacokinetics

Species	Dose	Route	T_1/2	CL	C_max	V_ss	AUC_last	T_max	F
Mice^[1]	1 mg/kg	i.v.	1.21 h	8.76 mL/min	1196.33 ng/mL	0.54 L/kg	1892.247 ng·h/mL	/	/
Mice^[1]	10 mg/kg	p.o.	/	/	2486.67 ng/mL	/	3666.208 ng·h/mL	0.5 h	19 %

In Vivo

GSPT1 degrader-8 (Compound 26) (30 mg/kg, p.o., daily for 17 days) inhibits tumor growth in NCI-N87 xenograft mice models^[1].

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

Animal Model:

NCI-N87 xenograft mice models^[1]
Dosage:

30 mg/kg
Administration:

Orally administration, daily for 17 days
Result:

Showed the tumor growth inhibition (TGI) rate of 93%.
Had no obvious weight loss and no death.

Chemical Information

Molecular Weight 453.49
Formula C₂₇H₂₃N₃O₄
SMILES

O=C(C1=CC2=C(CCC2)C=C1)NCC3=C4C5=C(N(C(CC6)C(NC6=O)=O)C(C5=CC=C4)=O)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]. Gao RD, et al. Identification of potent and orally bioavailable GSPT1 molecular glue degraders. Bioorg Med Chem Lett. 2025 Aug 16;129:130375. [Content Brief]

Calculators

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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.

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100 mg

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