Art. -Nr.: HY-170451

Seldegamadlin

(Synonyms: KT-253)

1 Cited Publications

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Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC₅₀ = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC₅₀ of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL).
(Pink: MDM-2/p53 ligand (HY-170452); Blue: Cereblon ligand (HY-163927); Black: linker (HY-W001478)).

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Reinheit: 98.53%
CAS. Nr.: 2713618-08-5
Formel: C₄₈H₅₂Cl₂FN₇O₆
Molecular Weight:912.87

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Seldegamadlin Chemical Structure

CAS. Nr.: 2713618-08-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC₅₀ = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC₅₀ of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL)^[1]^[2]^[3]^[4]. (Pink: MDM-2/p53 ligand (HY-170452); Blue: Cereblon ligand (HY-163927); Black: linker (HY-W001478)).

IC₅₀ & Target^[1]^[2]^[3]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

KT-253 degrades MDM2 with subnanomolar potency at concentrations of 0.01 nmol/L, 0.1 nmol/L, 1 Seldegamadlin (KT-253) inhibits cell viability of RS4;11 ALL cells with an IC₅₀ of 0.3 nM. The strong growth inhibition by KT-253 Is driven by the recruitment of both CRBN and MDM2^[3].
Seldegamadlin (1.8 nM; 2-4 h) inhibits MDM2 protein expression in RS4;11 ALL cells^[3].
Seldegamadlin (20 nM; 2-8 h) induces selective and temporal upregulation of p53 and its downstream targets in RS4;11 ALL cells^[3].
Brief exposure to Seldegamadlin (1-1000 nM; 4 h) is sufficient to trigger apoptosis in RS4;11 ALL cells^[3].
Seldegamadlin (0.01-10000 nM; 8 h) shows potent induction of p53 transcriptional gene targets, including MDM2, GDF15, CDKN1A, GADD45A, TNFRSF10B, FAS, and BBC3^[3].
Seldegamadlin (1-1000 nM; 4 h) resultes in a significantly lower percentage of cells in S-phase in RS4;11 and MV4;11 cells^[3].
Seldegamadlin (1-10,000 nM; 48-96 h) is active in various solid tumor cell lines including neuroblastoma, rhabdoid, eye, bile duct, colorectal, liposarcoma, gastric sarcoma, bone, breast, lung, prostate, liver, brain, kidney, thyroid, bladder, skin, ovarian, cervical, endometrial/uterine, head and neck, non-Cancerous, pancreatic^[4].

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

Western Blot Analysis^[3]

Cell Line:

RS4;11 cells
Concentration:

1.8 nM
Incubation Time:

2 h and 4 h
Result:

Led to potent and sustained MDM2 degradation to undetectable levels.

RT-PCR^[3]

Cell Line:

RS4;11 cells
Concentration:

20 nM
Incubation Time:

2 h, 4 h and 6 h
Result:

Showed the upregulation of p53, p21 and PHLDA3.

Apoptosis Analysis^[3]

Cell Line:

RS4;11 cells
Concentration:

1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time:

4 h
Result:

The 4-hour treatment was sufficient to induce apoptosis over a 48-hour time frame.

Cell Cycle Analysis^[3]

Cell Line:

RS4;11 and MV4;11 cells
Concentration:

1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time:

4 h
Result:

Resulted in a significantly lower percentage of cells in S-phase.

In Vivo

Seldegamadlin (KT-253) (1 mg/kg-10 mg/kg; IV) achieves sustained tumor regression in RS4;11 (ALL) and MV-4-11 (AML) xenograft mice models^[1].
Seldegamadlin (1-3 mg/kg; IV; once) triggeres rapid apoptosis and sustaines tumor regression in RS4;11 tumor–bearing mice^[3].
In the MOLM-13 subcutaneous xenograft model, the combination of Seldegamadlin (3 mg/kg; intravenous injection; single dose) and Venetoclax (HY-15531) overcame Venetoclax resistance^[3].
Seldegamadlin (3-10 mg/kg; IV; Q3W) inhibits tumor growth in multiple PDX solid tumor models, achieving complete responses^[4].

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

Animal Model:

Immuno-compromised host strain mice were subcutaneous with RS4;11 (ALL) cell lines^[1]
Dosage:

1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:

IV; once
Result:

Achieved sustained tumor regression in RS4;11 xenograft model.
Led to rapid increase in p53, p21 and PUMA (1 mg/kg).

Animal Model:

Female Balb/c nude mice were subcutaneously MV4;11 cells in the hind flank of the animals.^[3]
Dosage:

1 mg/kg, 3 mg/kg
Administration:

IV; once
Result:

Induced tumor regressions.
Demonstrated robust degradation of MDM2.
Showed an upregulation of proteomic biomarkers p53, p21, and PHLDA3.
Revealed robust upregulation of p53 and induction of apoptosis, as indicated by cleaved caspase-3 (CC-3) staining.
Led to robust activation of mRNA markers of both the intrinsic (BBC3) and extrinsic (TNFRSF10B and FAS) apoptotic pathways.

Animal Model:

Twenty-fourpediatric patient-derived xenograft (PDX) models (Ewing sarcoma, rhabdomyosarcoma, rhabdoid tumor,Wilms tumor, hepatoblastoma, and neuroblastoma, breast, lung,colorectal, gastric, melanoma) ^[4]
Dosage:

3 mg/kg, 10 mg/kg
Administration:

IV; Q3W; total 3 dose
Result:

Inhibited tumor growth in pediatric solid tumor models, achieving complete responses in 9 out of 24 models.

Animal Model:

Immuno-compromised host strain mice were subcutaneous with MV-4-11 (AML) cell lines^[1]
Dosage:

3 mg/kg
Administration:

IV; once every 3 weeks
Result:

Achieved sustained tumor regression in MV-4-11 xenograft model.
Led to rapid increase in GDF15, p21 and PUMA.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2713618-08-5
Appearance Solid
Molecular Weight 912.87
Formel C₄₈H₅₂Cl₂FN₇O₆
Color White to off-white
SMILES

ClC1=CC2=C([C@]3(C4(CCCCC4)N[C@@H](C(N[C@H]5CC[C@H](C(N6CCC(C7=CC=C8C(N(C)C(N8C9CCC(NC9=O)=O)=O)=C7)CC6)=O)CC5)=O)[C@@H]3C%10=C(F)C(Cl)=CC=C%10)C(N2)=O)C=C1
Synonyms

KT-253
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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bioRxiv

Ferrous Iron Accumulation Is a Hallmark and Therapeutic Vulnerability of Therapy-Induced Senescence. [Abstract]

2026 May 23:2026.05.20.726695. PMID: 42239384

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 95 mg/mL (104.07 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

1.0954 mL

5.4772 mL

10.9545 mL

5 mM

0.2191 mL

1.0954 mL

2.1909 mL

10 mM

0.1095 mL

0.5477 mL

1.0954 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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)

Verweise

[1]. Yogesh Chutake, KT-253, a highly potent and selective heterobifunctional MDM2 degrader for the treatment of wildtype p53 tumors with superior potency and differentiated biological activity compared to small molecule inhibitors (SMI).

[2]. Min Lu, et al. KT-253, a Highly Potent and Selective MDM2 Protein Degrader, Eliminates Malignant Myelofibrosis Stem/Progenitor Cells. Blood. Volume 144, Supplement 1, 5 November 2024, Page 3588.

[3]. Chutake YK, et al. KT-253, a Novel MDM2 Degrader and p53 Stabilizer, Has Superior Potency and Efficacy than MDM2 Small-Molecule Inhibitors. Mol Cancer Ther. 2025;24(4):497-510. [Content Brief]

[4]. Nancy Dumont, et al. Predictive Markers of Response to the MDM2 Degrader KT-253.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0954 mL	5.4772 mL	10.9545 mL	27.3862 mL
	5 mM	0.2191 mL	1.0954 mL	2.1909 mL	5.4772 mL
	10 mM	0.1095 mL	0.5477 mL	1.0954 mL	2.7386 mL
	15 mM	0.0730 mL	0.3651 mL	0.7303 mL	1.8257 mL
	20 mM	0.0548 mL	0.2739 mL	0.5477 mL	1.3693 mL
	25 mM	0.0438 mL	0.2191 mL	0.4382 mL	1.0954 mL
	30 mM	0.0365 mL	0.1826 mL	0.3651 mL	0.9129 mL
	40 mM	0.0274 mL	0.1369 mL	0.2739 mL	0.6847 mL
	50 mM	0.0219 mL	0.1095 mL	0.2191 mL	0.5477 mL
	60 mM	0.0183 mL	0.0913 mL	0.1826 mL	0.4564 mL
	80 mM	0.0137 mL	0.0685 mL	0.1369 mL	0.3423 mL
	100 mM	0.0110 mL	0.0548 mL	0.1095 mL	0.2739 mL

Seldegamadlin

1 Cited Publications

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Seldegamadlin

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Publications Citing Use of MedChemExpress (MCE) Seldegamadlin

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Seldegamadlin

PROTAC Library

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Seldegamadlin

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Seldegamadlin Related Classifications

Art. -Nr.: HY-170451