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Art. -Nr.: HY-182922

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SD-965

SD-965 is a selective STAT3 PROTAC degrader with a DC₅₀ of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma.
(Pink: STAT3 Target protein ligand; Blue: Cereblon ligand (HY-W1009348); Black: linker (HY-W017522)).

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CAS. Nr.: 3054394-56-5
Formel: C₅₆H₆₅N₁₀O₁₇PS
Molecular Weight:1213.21

Speicherung:

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

SD-965 Chemical Structure

CAS. Nr.: 3054394-56-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SD-965 is a selective STAT3 PROTAC degrader with a DC₅₀ of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma^[1]. (Pink: STAT3 Target protein ligand; Blue: Cereblon ligand (HY-W1009348); Black: linker (HY-W017522)).

IC₅₀ & Target^[1]

STAT3

0.14 μM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

In Vitro

SD-965 (up to 5 μM; 24 h) potently degrades STAT3 in the STAT3 HiBiT assay with a DC₅₀ of 0.14 μM and 85% maximal degradation after 24 h incubation^[1].
SD-965 potently inhibits the growth of MOLM-16 leukemia cells (IC₅₀ = 1.3 nM) and SU-DHL-1 lymphoma cells (IC₅₀ = 260 nM)^[1].
SD-965 (3.2-2000 nM; 14 h) selectively degrades STAT3 with >90% maximal degradation in human PBMCs after 14 h incubation, with no significant effect on other STAT family proteins up to 2 μM^[1].
SD-965 exhibits excellent microsomal and plasma stability in mouse, rat, dog, monkey, and human, with a half-life of >120 min in all tested matrices^[1].

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

Western Blot Analysis^[1]

Cell Line:

SU-DHL-1 human anaplastic large cell lymphoma cells
Concentration:

3.2-2000 nM
Incubation Time:

14 h
Result:

Degraded STAT3 with a DC₅₀ of 80 nM and a Dₘₐₓ of >90%.
Showed no obvious effect on STAT1 or STAT6, modestly reduced STAT2 and STAT5 at 2 μM, and increased STAT4 levels in a dose-dependent manner.

In Vivo

SD-965 (25-50 mg/kg; i.v.; once weekly; for 3-4 consecutive weeks) effectively inhibits tumor growth in SU-DHL-1 lymphoma xenograft mouse models^[1].

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

Animal Model:

SU-DHL-1 lymphoma xenograft mouse model^[1]
Dosage:

25-50 mg/kg
Administration:

i.v.; once weekly; for 3-4 consecutive weeks
Result:

Induced a maximum tumor regression by 58% at 25 mg/kg.
Reduced the tumor volume by 52% on day 5 after the first dose and by 96% on day 16, with 60% of mice without palpable tumors (50 mg/kg).

Chemical Information

CAS. Nr. 3054394-56-5
Molecular Weight 1213.21
Formel C₅₆H₆₅N₁₀O₁₇PS
SMILES

O=C(P(O)(O)=O)C1=CC2=C(NC(C(N[C@H]3CN(C(CCCCC(N4C[C@@]5([H])N(C6=C(OC5)C7=C(C(N([C@@H](CC8)C(NC8=O)=O)C7)=O)C=C6)CC4)=O)=O)CC[C@](CC[C@H]9C(N[C@@H](CCC(N)=O)COC%10=CC=CC(S(=O)(C)=O)=C%10)=O)([H])N9C3=O)=O)=C2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wu D, et al. Discovery of SD-965 as a Potent, Selective, and Efficacious STAT3 PROTAC Degrader. J Med Chem. 2026 Apr 9;69(7):8364-8387. [Content Brief]

Calculators

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)}

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.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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SD-965

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

SD-965 Related Classifications

HY-182922 Related Classifications