| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| S647571-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,700.90 |
| Specifications & Purity | 98% |
|---|---|
| Storage Temp | Store at -20°C,Argon charged |
| Shipped In | Ice chest + Ice pads |
| Product Description | SD-36 is a potent and efficacious STAT3 PROTAC degrader ( K d =~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 ( IC 50 =10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase In Vitro SD-36 inhibits the growth of a subset of acute myeloid leukemia and anaplastic large-cell lymphoma cell lines by inducing cell-cycle arrest and/or apoptosis. SD-36 (0.005-5 μM; 4 days) demonstrates potent activity (IC 50 ＜2 μM) in MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines. SD-36 (1 μM; 5 hours) completely depletes both monomeric and dimeric STAT3 protein in MOLM-16 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines Concentration: 0.005, 0.05, 0.5, 5 μM Incubation Time: 4 days Result: Demonstrated potent activity (IC 50 ＜2 μM) in those cell lines. Western Blot AnalysisCell Line: MOLM-16 cells Concentration: 1 μM Incubation Time: 5 hours Result: Completely depletes both monomeric and dimeric STAT3 protein. In Vivo SD-36 (25-100 mg/kg; i.v.; weekly dosing for 4 weeks) achieves complete and long-lasting tumor regression in mice . SD-36 effectively inhibits tumor growth at 25 and 50 mg/kg administered on day 1, 3, and 5 per week and achieved complete tumor regression at 100 mg/kg with the same schedule in the SU-DHL-1 xenograft model . SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID female mice (MOLM-16 xenograft model) Dosage: 25, 50, 100 mg/kg Administration: i.v.; weekly dosing for 4 weeks Result: At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression. Form:Solid IC50& Target:STAT3 50 nM (Kd) Cereblon |
| IUPAC Name | [4-[[[(2S)-2-[[(5S,8S,10aR)-5-[[5-(difluoromethyl)-1H-indole-2-carbonyl]amino]-3-[8-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]oct-7-ynoyl]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carbonyl]amino]-5-amino-5-oxopentanoyl]amino]-phenylmethyl]phenyl]phosphonic acid |
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| INCHI | InChI=1S/C59H62F2N9O12P/c60-53(61)37-18-22-43-38(30-37)31-45(63-43)55(75)65-46-33-68(51(73)15-8-3-1-2-5-10-34-13-9-14-41-42(34)32-69(58(41)78)47-25-27-50(72)66-56(47)76)29-28-39-19-24-48(70(39)59(46)79)57(77)64-44(23-26-49(62)71)54(74)67-52(35-11-6-4-7-12-35)36-16-20-40(21-17-36)83(80,81)82/h4,6-7,9,11-14,16-18,20-22,30-31,39,44,46-48,52-53,63H,1-3,8,15,19,23-29,32-33H2,(H2,62,71)(H,64,77)(H,65,75)(H,67,74)(H,66,72,76)(H2,80,81,82)/t39-,44+,46+,47?,48+,52?/m1/s1 |
| InChi Key | PHBGXRGBBVWZKA-QLXWUKDQSA-N |
| Canonical SMILES | C1CC(N2C1CCN(CC(C2=O)NC(=O)C3=CC4=C(N3)C=CC(=C4)C(F)F)C(=O)CCCCCC#CC5=C6CN(C(=O)C6=CC=C5)C7CCC(=O)NC7=O)C(=O)NC(CCC(=O)N)C(=O)NC(C8=CC=CC=C8)C9=CC=C(C=C9)P(=O)(O)O |
| PubChem CID | 156588550 |
| Molecular Weight | 1158.15 |
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| Solubility | DMSO : 150 mg/mL (129.52 mM; Need ultrasonic) |
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