Seldegamadlin
Based on 1 publication(s) in Google Scholar
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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- 純度: 98.53%
- CAS 番号: 2713618-08-5
- 分子式: C48H52Cl2FN7O6
- 分子量:912.87
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Seldegamadlin
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生物活性
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Cereblon |
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.
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Cell Line:RS4;11 cells
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Concentration:1.8 nM
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Incubation Time:2 h and 4 h
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Result:Led to potent and sustained MDM2 degradation to undetectable levels.
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Cell Line:RS4;11 cells
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Concentration:20 nM
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Incubation Time:2 h, 4 h and 6 h
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Result:Showed the upregulation of p53, p21 and PHLDA3.
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Cell Line:RS4;11 cells
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Concentration:1 nM, 10 nM, 100 nM, 1000 nM
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Incubation Time:4 h
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Result:The 4-hour treatment was sufficient to induce apoptosis over a 48-hour time frame.
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Cell Line:RS4;11 and MV4;11 cells
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Concentration:1 nM, 10 nM, 100 nM, 1000 nM
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Incubation Time:4 h
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Result:Resulted in a significantly lower percentage of cells in S-phase.
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.
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Animal Model:Immuno-compromised host strain mice were subcutaneous with RS4;11 (ALL) cell lines[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:IV; once
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Result:Achieved sustained tumor regression in RS4;11 xenograft model.
Led to rapid increase in p53, p21 and PUMA (1 mg/kg).
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Animal Model:Female Balb/c nude mice were subcutaneously MV4;11 cells in the hind flank of the animals.[3]
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Dosage:1 mg/kg, 3 mg/kg
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Administration:IV; once
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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.
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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]
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Dosage:3 mg/kg, 10 mg/kg
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Administration:IV; Q3W; total 3 dose
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Result:Inhibited tumor growth in pediatric solid tumor models, achieving complete responses in 9 out of 24 models.
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Animal Model:Immuno-compromised host strain mice were subcutaneous with MV-4-11 (AML) cell lines[1]
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Dosage:3 mg/kg
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Administration:IV; once every 3 weeks
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Result:Achieved sustained tumor regression in MV-4-11 xenograft model.
Led to rapid increase in GDF15, p21 and PUMA.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2713618-08-5
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性状 Solid
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分子量 912.87
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分子式 C48H52Cl2FN7O6
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Color White to off-white
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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
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別名
KT-253
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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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
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (284 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
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 (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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 関連分類
製品番号: HY-170451
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- Seldegamadlin
- 2713618-08-5
- KT-253
- KT253
- KT 253
- PROTACs
- MDM-2/p53
- Apoptosis
- Uveal melanoma
- biological activity
- potency
- xenograft model
- AML
- small molecule inhibitors
- solid tumors
- tumor cell killing
- p53 stabilization
- wildtype p53 tumors
- protein degradation
- apoptosis
- MDM2
- hematologic tumors
- autoregulatory feedback loop
- SMI
- tumor regression
- MDM2 degrader
- p53
- venetoclax resistance
- tumor suppression
- Inhibitor
- inhibitor
- inhibit