2. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs STAT
  4. SD-436

SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma (Pink: STAT3 ligand (HY-169361); Blue: E3 ligase ligand (HY-43722); Black: linker (HY-147052).

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

SD-436

SD-436 Chemical Structure

CAS No. : 2497585-50-7

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Based on 1 publication(s) in Google Scholar

SD-436 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

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Description

SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma (Pink: STAT3 ligand (HY-169361); Blue: E3 ligase ligand (HY-43722); Black: linker (HY-147052)[1].

IC50 & Target[1]

Cereblon

 

STAT3

19 nM (IC50)

STAT1

270 nM (IC50)

STAT5

>10 μM (IC50)

STAT6

>10 μM (IC50)

In Vitro

SD-436 (4 day treatment) inhibits the growth of MOLM-16 leukemia cell line, SU-DHL-1 and SUP-M2 lymphoma cell lines, with IC50 of 0.038 μM (MOLM-16), 0.43 μM (SU-DHL-1) and 0.39 μM (SUP-M2)[1].
SD-436 (0.1 nM-40 μM, 4 or 20 h) selectively reduces the levels of STAT3 protein in human PBMCs, SU-DHL-1 and MOLM-16 cell line (4 h)[1].
SD-436 (0.1 nM-40 μM, 20 h) effectively reduces the levels of the mutated STAT3 protein (STAT3K658R) in a dose-dependent manner in the Pfeiffer cell line, with a DC50 value of 2.5 nM[1].
SD-436 shows excellent stability in mouse, rat, dog, monkey and human plasma, with T1/2 of >120 min[1].
SD-436 has no significant inhibition of the human ether-a-go-go-related gene potassium channels (hERG inhibition: 1.3% for 3μM and 1.1% for 30 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SD-436 Related Antibodies

Western Blot Analysis[1]

Cell Line: PBMC, MOLM-16, SU-DHL-1 and Pfeiffer
Concentration: 0.1 nM, 0.5 nM, 2.5 nM, 13 nM, 64 nM, 320 nM, 1600 nM, 8000 nM, 40000 nM
Incubation Time: 20 h
Result: Reduced the levels of STAT3 protein in human PBMCs and SU-DHL-1 cell line, with DC50 of 0.1 nM and 10 nM, respectively.
Achieved near complete degradation at 320 nM with merely a 4 h treatment time in the MOLM-16 cell line.
Reduced the levels of the mutated STAT3 protein in a dose-dependent manner in the Pfeiffer cell line, with a DC50 value of 2.5 nM.
Showed high selectivity for STAT3 over other STAT proteins.
In Vivo

SD-436 (5 mg/kg, i.v., single) effectively induces rapid, complete, and durable depletion of STAT3 in mouse native (liver and spleen) and MOLM-16 xenograft tumor tissues[1].
SD-436 (5-25 mg/kg, i.v.) shows antitumor activity in leukemia and lymphoma xenograft models in mice[1].
Pharmacokinetics of SD-436 in mice, rats, and dogs

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Species IV dose (mg/kg) t1/2 (h) Cmax (ng/mL) AUC(0-t) (h × ng/mL) Vz (L/kg) CI (mL/min/kg) Cl (%HBF)
ICR mouse 5 22.1 130,185 859,223 0.10 0.051 0.1%
SD rat 5 1.0 82,626 59,484 0.12 1.4 2.6%
beagle dog 1 2.3 8861 10,699 0.29 1.5 2.7%
Animal Model: MOLM-16 acute leukemia xenograft model and the SU-DHL-1 lymphoma xenograft model in SCID mice (injected subcutaneously with 3 × 106 MOLM-16 cells or 5 × 106 SU-DHL-1 cells)[1]
Dosage: 5, 10, 20 mg/kg (MOLM-16); 10, 25 mg/kg (SU-DHL-1)
Administration: Intravenous injection (i.v.); once a week, four weeks (MOLM-16: 5, 10, 20 mg/kg; SU-DHL-1: 10, 25 mg/kg) or twice a week, four weeks (SU-DHL-1: 25 mg/kg)
Result: Showed that SD-436 at 5 mg/kg was able to achieve a maximum of 76% tumor regression in the MOLM-16 leukemia xenograft model.
Induced complete tumor regression at 10 and 20 mg/kg in the MOLM-16 leukemia xenograft model.
Achieved complete and long-lasting tumor regression in the SU-DHL-1 xenograft model at 25 mg/kg weekly dosing schedule.
Molecular Weight

1248.20

Formula

C58H62F4N9O14PS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1[C@H](CN(CC[C@@H]2N1[C@@H](CC2)C(N[C@@H](CCC(N)=O)C(N[C@H](C(N3CCC(CC3)CCC#CC4=CC=CC5=C4CN(C5=O)C6CCC(NC6=O)=O)=O)CC7=CC=C(C(F)=C7)F)=O)=O)C(OC)=O)NC(C8=CC9=C(S8)C=CC(C(F)(P(O)(O)=O)F)=C9)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (80.12 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 0.8012 mL 4.0058 mL 8.0115 mL
5 mM 0.1602 mL 0.8012 mL 1.6023 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; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8012 mL 4.0058 mL 8.0115 mL 20.0288 mL
5 mM 0.1602 mL 0.8012 mL 1.6023 mL 4.0058 mL
10 mM 0.0801 mL 0.4006 mL 0.8012 mL 2.0029 mL
15 mM 0.0534 mL 0.2671 mL 0.5341 mL 1.3353 mL
20 mM 0.0401 mL 0.2003 mL 0.4006 mL 1.0014 mL
25 mM 0.0320 mL 0.1602 mL 0.3205 mL 0.8012 mL
30 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.6676 mL
40 mM 0.0200 mL 0.1001 mL 0.2003 mL 0.5007 mL
50 mM 0.0160 mL 0.0801 mL 0.1602 mL 0.4006 mL
60 mM 0.0134 mL 0.0668 mL 0.1335 mL 0.3338 mL
80 mM 0.0100 mL 0.0501 mL 0.1001 mL 0.2504 mL
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SD-436 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-4362497585-50-7SD436SD 436PROTACsSTATLeukemiaLymphomaMOLM-16ICRPermeabilityXenograftInhibitorinhibitorinhibit

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