SMD-3236
SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia.
(Pink: SMARCA2 ligand (HY-170817); Blue: VHL ligand (HY-170826); Black: linker (HY-170825)).
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- No. CAS: 3033586-31-8
- Fòrmula: C61H75ClN10O5S
- Peso molecular:1095.83
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
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VHL |
SMARCA2 |
SMD-3236 (Compound 22) potently inhibits the proliferation of SMARCA4-deficient cell lines, with GI50 values of 1.5 nM (SK-Mel-5), 9.5 nM (NCI-H838), 2.2 nM (NCI-H1568), 9.8 nM (NCI-H1944) and 4.8 nM (NCI-H1693) (Imax: 71-95%), whereas it exhibits only extremely low activity in SMARCA4 wild-type cell lines (GI50 >10 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SMD-3236 (30 mg/kg; i.v.; single dose) reduces SMARCA2 protein levels by up to 97% for at least 168 h in MV4-11 xenograft tumors in SCID mice, while increasing SMARCA4 protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB.17 SCID (female, 6-8 weeks old)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.v.; weekly; 3 weeks
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Result:Inhibited tumor growth by 87% compared to vehicle control.
Inhibited tumor growth by 91% compared to vehicle control.
Induced minimal tumor growth after treatment cessation.
Caused no significant weight loss or other signs of toxicity throughout the experiment.
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Animal Model:CB.17 SCID (female, 6-10 weeks old)[1]
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Dosage:30 mg/kg
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Administration:i.v.; single dose
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Result:Reduced SMARCA2 protein levels in MV4-11 tumors by 97% at 24 h post-administration.
Reduced SMARCA2 protein levels in MV4-11 tumors by 85% at 96 h post-administration.
Reduced SMARCA2 protein levels in MV4-11 tumors by 89% at 168 h post-administration.
Increased SMARCA4 protein levels in MV4-11 tumors by 131% at 24 h post-administration.
Increased SMARCA4 protein levels in MV4-11 tumors by 110% at 96 h post-administration.
Increased SMARCA4 protein levels in MV4-11 tumors by 45% at 168 h post-administration.
Chemical Information
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No. CAS 3033586-31-8
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Peso molecular 1095.83
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Fòrmula C61H75ClN10O5S
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SMILES
ClC1=CC=CC(N(C(C=C(C2CCN(C[C@H]3CC[C@H](C4=CN([C@@H](C(C)(C)C)C(N5[C@H](C(N[C@@H](CN6CCOCC6)C7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C5)=O)N=N4)CC3)CC2)C=C9)=C9C%10%11CCCCC%11)C%10=N%12)=C1C%12=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SMD-3236 Related Classifications
HY-170824 Related Classifications
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