SD-36 |
| Catalog No.GC61270 |
SD-36 es un degradador de STAT3 PROTAC potente y eficaz (Kd=~50 nM) y demuestra una alta selectividad sobre otros miembros de STAT. SD-36 también degrada eficazmente las proteÍnas STAT3 mutadas en las células y suprime la actividad transcripcional de STAT3 (IC50 = 10 nM). SD-36 ejerce una sÓlida actividad antitumoral y logra una regresiÓn tumoral completa y duradera en modelos de tumores de ratÓn. SD-36 estÁ compuesto por el inhibidor de STAT3 SI-109, un enlazador y un anÁlogo del ligando de Cereblon Lenalidomida para la ubiquitina ligasa E3.
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 |
| Solubility | 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 | |||
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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 |
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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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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