Art. -Nr.: HY-154860

PTD10

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PTD10 is a selective and potent BTK PROTAC degrader (DC₅₀ = 0.5 nM, K_D = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease.
(Pink: Btk ligand (HY-19834); Blue: Cereblon ligand (HY-14658); Black: linker (HY-Y0966)).

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Reinheit: 97.38%
CAS. Nr.: 2642231-19-2
Formel: C₄₉H₅₁N₁₁O₈
Molecular Weight:922.00

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PTD10 Chemical Structure

CAS. Nr.: 2642231-19-2

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

PTD10 is a selective and potent BTK PROTAC degrader (DC₅₀ = 0.5 nM, K_D = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease^[1]. (Pink: Btk ligand (HY-19834); Blue: Cereblon ligand (HY-14658); Black: linker (HY-Y0966)).

IC₅₀ & Target^[1]

Cereblon

Caspase 3

Bcl-2

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
TMD8	IC₅₀	1.4 nM Compound: PTD10	Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay	[PMID: 37195170]

In Vitro

PTD10 (0.15-3000 nM; 17 h) potently degrades BTK via the CRBN-dependent ubiquitin-proteasome pathway in Ramos cells (DC₅₀ = 0.5 nM) and JeKo-1 cells (DC₅₀ = 0.6 nM), with maximal degradation exceeding 95% in both cell lines^[1].
PTD10 binds to purified BTK with a K_d of 2.28 nM^[1].
PTD10 (2 h) engages intracellular BTK (IC₅₀ = 97 nM) and CRBN (IC₅₀ = 107 nM) in HEK293 cells, with positive cooperativity in BTK binding^[1].
PTD10 efficiently promotes ternary complex formation between BTK and CRBN in HEK293 cells, achieving 100% maximal BRET signal^[1].
PTD10 is a highly selective BTK degrader in TMD8 cells, with no significant off-target degradation of other tested kinases, while degrading neo-substrates IKZF1, IKZF3, and ZNF280D without affecting GSPT1^[1].
PTD10 (0.1-10000 nM; 48 h) potently inhibits growth of TMD8 cells (IC₅₀ = 1.4 nM) and Mino cells (IC₅₀ = 2.2 nM)^[1].
PTD10 (0.15-3000 nM; 48 h) induces dose-dependent apoptosis in TMD8 and Mino cells via activation of the caspase-dependent and mitochondrial pathways^[1].
PTD10 (0.15-3000 nM; 48 h) potently inhibits the BCR signaling pathway in TMD8 and Mino cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Ramos, JeKo-1 B-cell lymphoma cell lines
Concentration:

0.15, 0.45, 1.4, 4, 12, 37, 111, 333, 1000, 3000 nM
Incubation Time:

17 h
Result:

Potently degraded BTK in both cell lines, with a DC₅₀ of 0.5 nM (Dmax 97.1%) in Ramos cells and 0.6 nM (Dmax 95.7%) in JeKo-1 cells.
Completely blocked BTK degradation when cotreated with GDC-0853 (HY-19834) or Iberdomide (HY-101291).
Inhibited BTK degradation when pretreated with Bortezomib (HY-10227) or MLN-4924 (HY-70062).

Apoptosis Analysis^[1]

Cell Line:

TMD8, Mino B-cell lymphoma cell lines
Concentration:

0.15, 0.45, 1.4, 4, 12, 37, 111, 333, 1000, 3000 nM
Incubation Time:

48 h
Result:

Induced apoptosis in a dose-dependent manner in both cell lines, with robust apoptosis detected at 333 nM (a Hook effect was observed at higher concentrations).

Western Blot Analysis^[1]

Cell Line:

TMD8, Mino B-cell lymphoma cell lines
Concentration:

0.15, 0.45, 1.4, 4, 12, 37, 111, 333, 1000, 3000 nM
Incubation Time:

48 h
Result:

Caused dose-dependent decreases in full-length PARP, caspase-3, Bcl-2, and MCL-1, with corresponding increases in cleaved-PARP and cleaved-caspase-3.
Caused robust downregulation of phosphorylated BTK, PLCγ2, AKT, and NF-κB, as well as total PLCγ2, AKT, and NF-κB in both cell lines after 48 h.
Activated ERK phosphorylation in TMD8 cells but unaffected in Mino cells.

Chemical Information

CAS. Nr. 2642231-19-2
Appearance Solid
Molecular Weight 922.00
Formel C₄₉H₅₁N₁₁O₈
Color Light yellow to yellow
SMILES

O=C1N(C=C(C=C1NC2=NC=C(N3CCN(C[C@@H]3C)C(CNC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O)=O)C=C2)C7=CC=NC(N8CCN9C(C8=O)=CC%10=C9CC(C)(C%10)C)=C7CO)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (54.23 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

1.0846 mL

5.4230 mL

10.8460 mL

5 mM

0.2169 mL

1.0846 mL

2.1692 mL

10 mM

0.1085 mL

0.5423 mL

1.0846 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 (277 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Li YQ, et al. Discovery of Novel Bruton's Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy. J Med Chem. 2023;66(11):7454-7474. [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	1.0846 mL	5.4230 mL	10.8460 mL	27.1150 mL
	5 mM	0.2169 mL	1.0846 mL	2.1692 mL	5.4230 mL
	10 mM	0.1085 mL	0.5423 mL	1.0846 mL	2.7115 mL
	15 mM	0.0723 mL	0.3615 mL	0.7231 mL	1.8077 mL
	20 mM	0.0542 mL	0.2711 mL	0.5423 mL	1.3557 mL
	25 mM	0.0434 mL	0.2169 mL	0.4338 mL	1.0846 mL
	30 mM	0.0362 mL	0.1808 mL	0.3615 mL	0.9038 mL
	40 mM	0.0271 mL	0.1356 mL	0.2711 mL	0.6779 mL
	50 mM	0.0217 mL	0.1085 mL	0.2169 mL	0.5423 mL

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PTD10

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

PROTAC Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PTD10 Related Classifications

HY-154860 Related Classifications