2. PROTAC Apoptosis
  3. PROTACs MDM-2/p53 Apoptosis
  4. KT-253

KT-253 is a p53 stabilizer and a PROTAC degrader for MDM2 (DC50=0.4 nM). KT-253 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. KT-253 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))

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

KT-253 Chemical Structure

KT-253 Chemical Structure

CAS No. : 2713618-08-5

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Based on 1 publication(s) in Google Scholar

KT-253 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

KT-253 is a p53 stabilizer and a PROTAC degrader for MDM2 (DC50=0.4 nM). KT-253 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. KT-253 exhibits antitumor efficacy in mouse models[1]. (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))

Molecular Weight

912.87

Formula

C48H52Cl2FN7O6
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0954 mL 5.4772 mL 10.9545 mL
5 mM 0.2191 mL 1.0954 mL 2.1909 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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
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KT-253 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KT-2532713618-08-5KT253KT 253PROTACsMDM-2/p53ApoptosisRS4;11MOLM-13NOG mouseAMLInhibitorinhibitorinhibit

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