SD-36 |
カタログ番号GC61270
One-Click Copy Product Info
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SD-36 は、強力で有効な STAT3 PROTAC 分解剤 (Kd=~50 nM) であり、他の STAT メンバーよりも高い選択性を示します。 SD-36 はまた、細胞内の変異 STAT3 タンパク質を効果的に分解し、STAT3 の転写活性を抑制します (IC50=10 nM)。 SD-36 は強力な抗腫瘍活性を発揮し、マウス腫瘍モデルで完全かつ長期的な腫瘍退縮を達成します。 SD-36 は、STAT3 阻害剤 SI-109、リンカー、および E3 ユビキチン リガーゼのセレブロン リガンド レナリドマイドの類似体で構成されています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2429877-44-9
Sample solution is provided at 25 µL, 10mM.
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SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~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 (IC50=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 CRBN ligand Lenalidomide for E3 ubiquitin ligase[1].
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 (IC50<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]. Cell Viability Assay[1] Cell Line: MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines
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]. Animal Model: SCID female mice (MOLM-16 xenograft model)[1]
[1]. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17.
| Cas No. | 2429877-44-9 | SDF | |
| Canonical 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 | ||
| Formula | C59H62F2N9O12P | M.Wt | 1158.15 |
| 溶解度 | DMSO: 150 mg/mL (129.52 mM) | Storage | -20°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 863.4 μL | 4.3172 mL | 8.6345 mL |
| 5 mM | 172.7 μL | 863.4 μL | 1.7269 mL |
| 10 mM | 86.3 μL | 431.7 μL | 863.4 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)