[CAS NO. 2429877-44-9] SD-36
PRODUCTS SPECIFICATIONS [2429877-44-9]
DESCRIPTION [2429877-44-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1158.15 |
| Molecular Formula | C59H62F2N9O12P |
| SMILES | O=C([C@@H](NC([C@@H]1CC[C@H](CCN(C(CCCCCC#CC2=CC=CC3=C2CN(C4CCC(NC4=O)=O)C3=O)=O)C[C@@H]5NC(C6=CC(C=C(C(F)(P(O)(O)=O)F)C=C7)=C7N6)=O)N1C5=O)=O)CCC(N)=O)NC(C8=CC=CC=C8)C9=CC=CC=C9 |
1 Publications Citing Use of MCE
Summary
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 [1] .
IC50 & Target
|
STAT3 50 nM (Kd) |
Cereblon
|
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
[1]
.
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
[1]
.
SD-36 (1 μM; 5 hours) completely depletes both monomeric and dimeric STAT3 protein in MOLM-16 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell 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 Analysis [1]
| Cell 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
[1]
.
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
[1]
.
SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | SCID female mice (MOLM-16 xenograft model) [1] |
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 150 mg/mL ( 129.52 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.8634 mL | 4.3172 mL | 8.6345 mL |
| 5 mM | 0.1727 mL | 0.8634 mL | 1.7269 mL |
| 10 mM | 0.0863 mL | 0.4317 mL | 0.8634 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 5 mg/mL (4.32 mM); Clear solution