SD-36

Name: SD-36
Brand: MedChemExpress
SKU: HY-129602
Rating: 5.0 (9 reviews)

Cat. No.: HY-129602 Purity: 99.73%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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 (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 Cereblon ligand Lenalidomide for E3 ubiquitin ligase. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

CAS No. : 2429877-44-9

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE SD-36

RT-PCR

Cell Proliferation/Viability Assay

Cell Migration/Invasion Assay

Flow Cytometry

In Vivo Efficacy Study

IHC

: SD-36 purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2023 Jun 28;15(702):eabo3826. [Abstract]; qRT-PCR analysis of PIK3CD mRNA expression performed on ALK+ ALCL cell lines treated with SD-36 (1 μM). n = 3 technical replicates.

: SD-36 purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2023 Jun 28;15(702):eabo3826. [Abstract]; Western blot analysis on ALK+ ALCL human cell lines treated with SD-36 (1 μM).

: SD-36 purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2024 Jan 9;19(1):100-111. [Abstract]; GMP-like LSCs isolated from 3-cytokine-medium-cultured AML cells. GMP-like LSCs were starved for 4 h followed by 1 μM SD-36 (Stat3 PROTAC). Cells were subsequently stimulated by IL-3 or IL-6 for 30 min and collected for western blotting.

: SD-36 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Sep;25(17):8261-8270. [Abstract]; U87 and U251 cells were treated with increasing concentration of SD-36 or Stattic for 72 h. Cell viability was analysed by MTS assay.

: SD-36 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Sep;25(17):8261-8270. [Abstract]; Invasion of U87 and U251 cells treated with SD-36 (100 nM; 24 h) was analysed by Transwell assay. The results sowed that SD-36 treatment decreases cell invasion in U87 and U251 cells, which was detected by Transwell assay.

: SD-36 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Sep;25(17):8261-8270. [Abstract]; U87 and U251 cells were treated with 100 nmol/L SD-36 or 1 μmol/L Stattic for 24 h. Apoptosis was analysed by flow cytometry. The results sowed that SD-36 effectively enhanced apoptotic populations in the two cell lines.

: SD-36 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Sep;25(17):8261-8270. [Abstract]; U87 and U251 cells were treated with 100 nmol/L SD-36 or 1 μmol/L Stattic for 24 h. Indicated protein levels were analysed by western blotting. The results sowed that SD-36 treatment resulted in increase in E-cadherin and decrease in N-cadherin, vimentin and snail in U87 and U251 cells.

: SD-36 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Sep;25(17):8261-8270. [Abstract]; Tumour volume was quantified for established PDX tumours in NSG mice treated with vehicle, SD-36 (2 mg/kg/d; ip; twice a week), TMZ, or the combination of SD-36 and TMZ, and representative tumours were examined at the end of the experiment.

: SD-36 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2021 Sep;25(17):8261-8270. [Abstract]; Mcl‐1 and STAT3 expression level was analysed in the indicated tumours by IHC. Scale bars: 25 μm. The results SD-36 (2 mg/kg/d; ip; twice a week) treatment decreased Mcl-1 and STAT3 expression in PDX mouse tumours.

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Biological Activity
Purity & Documentation
References
Customer Review

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 (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 Cereblon ligand Lenalidomide for E3 ubiquitin ligase^[1]. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

STAT3

50 nM (Kd)

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
SU-DHL-1	IC₅₀	0.61 μM Compound: 14; SD-36	Antiproliferative activity against human SUDHL1 cells assessed as reduction in cell viability incubated for 4 days by cell-titer glo luminescent assay Antiproliferative activity against human SUDHL1 cells assessed as reduction in cell viability incubated for 4 days by cell-titer glo luminescent assay	[PMID: 31747516]
SU-DHL-1	IC₅₀	3.4 μM Compound: SD-36; 1	Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay	[PMID: 34141084]

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 (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].

MedChemExpress (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 (IC₅₀＜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].

MedChemExpress (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.

Molecular Weight

1158.15

Formula

C₅₉H₆₂F₂N₉O₁₂P

CAS No.

2429877-44-9

Appearance

Solid

Color

White to off-white

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

Shipping

Shipping with dry ice.

Storage

-80°C, stored under nitrogen

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (86.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (1.08 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (1.08 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (1.08 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.73%

Select Batch:

Data Sheet (283 KB) SDS (251 KB)

COA (254 KB) HNMR (428 KB) RP-HPLC (262 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.8634 mL	4.3172 mL	8.6345 mL	21.5861 mL
	5 mM	0.1727 mL	0.8634 mL	1.7269 mL	4.3172 mL
	10 mM	0.0863 mL	0.4317 mL	0.8634 mL	2.1586 mL
	15 mM	0.0576 mL	0.2878 mL	0.5756 mL	1.4391 mL
	20 mM	0.0432 mL	0.2159 mL	0.4317 mL	1.0793 mL
	25 mM	0.0345 mL	0.1727 mL	0.3454 mL	0.8634 mL
	30 mM	0.0288 mL	0.1439 mL	0.2878 mL	0.7195 mL
	40 mM	0.0216 mL	0.1079 mL	0.2159 mL	0.5397 mL
	50 mM	0.0173 mL	0.0863 mL	0.1727 mL	0.4317 mL
	60 mM	0.0144 mL	0.0720 mL	0.1439 mL	0.3598 mL
	80 mM	0.0108 mL	0.0540 mL	0.1079 mL	0.2698 mL

SD-36 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SD-362429877-44-9SD36SD 36PROTACsSTATApoptosisPROTACSH2 domaindegraderleukemialymphomatranscriptionalfactorapoptosislong-lastingInhibitorinhibitorinhibit

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SD-36

Customer Review

SD-36 Related Antibodies

9 Publications Citing Use of MCE SD-36

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References

Customer Review

SD-36 Related Antibodies

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Complete Stock Solution Preparation Table

SD-36 Related Classifications

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