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SD-436 is a selective and highly efficient STAT3 PROTAC degrader (DC50 = 0.5 μM), with an IC50 of 19 nM for STAT3, significantly higher than for STAT1/4/5/6. SD-436 depletes STAT3 and induces tumour regression in mouse leukaemia and lymphoma xenograft models.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $993 | In Stock | |
5 mg | $2,480 | In Stock | |
10 mg | $3,980 | In Stock | |
25 mg | $7,670 | In Stock | |
50 mg | $9,870 | In Stock |
Description | SD-436 is a selective and highly efficient STAT3 PROTAC degrader (DC50 = 0.5 μM), with an IC50 of 19 nM for STAT3, significantly higher than for STAT1/4/5/6. SD-436 depletes STAT3 and induces tumour regression in mouse leukaemia and lymphoma xenograft models. |
Targets&IC50 | STAT3:19 nM, STAT1:270 nM, STAT6:>10 μM, STAT5:>10 μM |
In vitro | Methods: Human PBMC, SU-DHL-1, and MOLM-16 cell lines were treated with SD-436 (0.1 nM-40 μM, 20 h), and the expression level of STAT3 protein in the cells was detected by Western blot. Results: SD-436 could reduce the level of STAT3 protein in human PBMC, SU-DHL-1, and MOLM-16 cell lines. [1] |
In vivo | SD-436 (5-25 mg/kg, intravenous) was used to treat mice bearing leukemia and lymphoma xenografts and was found to exhibit antitumor activity in mice. [1] |
Synonyms | SD436 |
Molecular Weight | 1248.2 |
Formula | C58H62F4N9O14PS |
Cas No. | 2497585-50-7 |
Smiles | C(#CCCC1CCN(C([C@H](CC2=CC(F)=C(F)C=C2)NC([C@@H](NC(=O)[C@H]3N4[C@](CC3)(CCN(C(OC)=O)C[C@H](NC(=O)C5=CC=6C(S5)=CC=C(C(P(=O)(O)O)(F)F)C6)C4=O)[H])CCC(N)=O)=O)=O)CC1)C7=C8C(C(=O)N(C8)C9C(=O)NC(=O)CC9)=CC=C7 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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