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Art. -Nr.: HY-169360

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SD-436

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Based on 1 Customer Validation

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: Cereblon ligand (HY-43722); Black: linker (HY-147052)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.27%
CAS. Nr.: 2497585-50-7
Formel: C₅₈H₆₂F₄N₉O₁₄PS
Molecular Weight:1248.20

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

SD-436 Chemical Structure

CAS. Nr.: 2497585-50-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: STAT3 ligand (HY-169361); Blue: Cereblon ligand (HY-43722); Black: linker (HY-147052)).

IC₅₀ & Target^[1]

Cereblon

STAT3

19 nM (IC₅₀)

STAT1

270 nM (IC₅₀)

STAT5

>10 μM (IC₅₀)

STAT6

>10 μM (IC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

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 (STAT3^K658R) 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 T_1/2 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.

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.

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.

Chemical Information

CAS. Nr. 2497585-50-7
Appearance Solid
Molecular Weight 1248.20
Formel C₅₈H₆₂F₄N₉O₁₄PS
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Species	IV dose (mg/kg)	t_1/2 (h)	C_max (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%

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8012 mL

4.0058 mL

8.0115 mL

5 mM

0.1602 mL

0.8012 mL

1.6023 mL

10 mM

0.0801 mL

0.4006 mL

0.8012 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xu, et al. Discovery of SD-436: A Potent, Highly Selective and Efficacious STAT3 PROTAC Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression. Journal of medicinal chemistry. 2024, 67(22), 20495–20513. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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SD-436

PROTAC Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SD-436 Related Classifications

HY-169360 Related Classifications