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 No.: 3054394-56-5
- Formule: C56H65N10O17PS
- Masse moléculaire:1213.21
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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STAT3 0.14 μM (DC50) |
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.
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Cell Line:SU-DHL-1 human anaplastic large cell lymphoma cells
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Concentration:3.2-2000 nM
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Incubation Time:14 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SU-DHL-1 lymphoma xenograft mouse model[1]
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Dosage:25-50 mg/kg
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Administration:i.v.; once weekly; for 3-4 consecutive weeks
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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
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CAS No. 3054394-56-5
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Masse moléculaire 1213.21
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Formule C56H65N10O17PS
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SD-965 Related Classifications
HY-182922 Related Classifications
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