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Cat. No.: HY-184896

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XYD113

Name: XYD113
Brand: MedChemExpress
SKU: HY-184896
Availability: PreOrder

XYD113 is an orally active, selective GSPT1 Molecular glue degrader. XYD113 promotes the formation of the CRBN-GSPT1 ternary complex and mediates GSPT1 degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. XYD113 downregulates genes associated with the occurrence and progression of prostate cancer (c-Myc, AR, AR-V7, KLK3, KLK2, TMPRSS2). XYD113 exhibits anticancer activity against prostate cancer. XYD113 can be used in the research of prostate cancer.

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CAS No.: 3032314-99-8
화학식: C₂₁H₂₁ClN₄O₄
분자량:428.87

보관:

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

XYD113 Chemical Structure

CAS No.: 3032314-99-8

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수량

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

eRF3a/GSPT1

AR-V7

KLK3

KLK2

TMPRSS2

CRBN

All Eukaryotic Release Factor (eRF) Isoforms :

All Kallikrein Isoforms :

In Vitro

Anti-cancerOthers

Anti-cancer

XYD113 (96 h) potently inhibits the proliferation of 22Rv1 cells, with an IC₅₀ of 69 nM^[1].
XYD113 (12-1000 nM; 1-12 h) induces dose- and time-dependent degradation of GSPT1 in 22Rv1 cells, with potency comparable to that of MRT-2359 (HY-153356); meanwhile, this compound shows high selectivity, as it does not degrade SALL4, IKZF1/2/3, ZFP91 or CK1α even at a concentration of 1 μM^[1].
XYD113 (100-500 nM; 12 h) effectively downregulates the expression of genes critical for prostate cancer initiation and progression in 22Rv1 cells when applied at concentrations of 100 nM and 500 nM for 12 h^[1].

Others

As a molecular glue, XYD113 (0.1-100 μM; 1.5 h) promotes the formation of the CRBN-GSPT1 ternary complex in a concentration-dependent manner^[1].

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

Cell Viability Assay^[1]

Cell Line:

human prostate cancer 22Rv1 cells
Concentration:

range of concentrations
Incubation Time:

96 h
Result:

Potently inhibited 22Rv1 cell proliferation with an IC₅₀ of 69 nM.

Western Blot Analysis^[1]

Cell Line:

human prostate cancer 22Rv1 cells
Concentration:

12-1000 nM (6 h incubation); 100 nM (1-12 h incubation); 1 μM (6 h incubation)
Incubation Time:

6 h (12-1000 nM, 1 μM); 1-12 h (100 nM)
Result:

Induced complete degradation of GSPT1 at 1 μM after 6 h.
Reduced GSPT1 protein levels in a dose-dependent manner across 12-1000 nM after 6 h.
Reduced GSPT1 protein levels in a time-dependent manner across 1-12 h at 100 nM.
Showed no significant degradation of off-target substrates SALL4, IKZF1, IKZF2, IKZF3, ZFP91, or CK1α even at 1 μM after 6 h.

Real Time qPCR^[1]

Cell Line:

human prostate cancer 22Rv1 cells
Concentration:

100-500 nM
Incubation Time:

12 h
Result:

Significantly downregulated mRNA expression levels of c-Myc, AR, AR-V7, KLK3, KLK2, and TMPRSS2.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-t	AUC_0-∞	T_1/2	CL	F
Rat^[1]	1 mg/kg	i.v.	2250 ng/mL	0.08 h	1341 ng·h/mL	1345 ng·h/mL	1.71 h	757 mL/h/kg	/
Rat^[1]	5 mg/kg	p.o.	128 ng/mL	1.00 h	499 ng·h/mL	538 ng·h/mL	2.73 h	/	7.45 %

In Vivo

Anti-cancer

XYD113 (5 mg/kg; p.o.; daily; 21 days) achieves 46% tumor growth inhibition in BALB/c-nude mice bearing 22Rv1 xenografts, with a favorable safety profile^[1].

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

Animal Model:

BALB/c-nude (5 weeks old)^[1]
Dosage:

5 mg/kg
Administration:

p.o.; daily; 21 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 46%.
Showed no significant body weight loss during treatment.
Caused significant downregulation of GSPT1 protein levels in harvested tumor tissues.
Revealed no tissue abnormalities in major organs (heart, liver, spleen, lung, kidney) compared to vehicle control.

Chemical Information

CAS No. 3032314-99-8
분자량 428.87
화학식 C₂₁H₂₁ClN₄O₄
SMILES

ClC1=CC(NC(NCC2=CC=CC(C(NC3CCC(NC3=O)=O)=O)=C2)=O)=CC=C1C
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Shen H, et al. Development of XYD113 as a potent and highly selective GSPT1 degrader for cancer therapy. Acta pharmacologica Sinica. 2026 Jun 23. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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XYD113

All Eukaryotic Release Factor (eRF) Isoforms

All Kallikrein Isoforms