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Art. -Nr.: HY-153361

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YD23

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YD23 is a selective SMARCA2 PROTAC degrader with DC₅₀ values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC).
(Pink: SMARCA2 ligand (HY-44012); Blue: Cereblon ligand (HY-41547); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.80%
CAS. Nr.: 2951015-29-3
Formel: C₃₈H₃₉FN₈O₇
Molecular Weight:738.76

Speicherung:

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

YD23 Chemical Structure

CAS. Nr.: 2951015-29-3

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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

YD23 is a selective SMARCA2 PROTAC degrader with DC₅₀ values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC)^[1]^[2]. (Pink: SMARCA2 ligand (HY-44012); Blue: Cereblon ligand (HY-41547); Black: linker).

IC₅₀ & Target^[2]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle SWI/SNF Complex Isoform-spezifische Produkte anzeigen :

In Vitro

YD23 (0.0001-10 μM, 12 days) selectively inhibits growth of SMARCA4-mutant ung cancer cell lines compared to SMARCA4-WT cells (median IC₅₀ of 0.11 μM and 6.0 μM, for each group, respectively)^[2].
YD23 (1 μM, 96 h)-downregulated genes are significantly enriched in cell cycle-related pathways such as E2F target genes, G2/M checkpoint, and mitotic spindle^[2].

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

In Vivo

YD23 (12.5 mg/kg, i.p., once daily for 25-26 days) has demonstrates strong anti-tumor activity in tumor xenografts of three SMARCA4-mutated lung cancers in mice^[1].

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

Animal Model:

Human tumor xenografts of three SMARCA4-mutated lung cancers (H1568, H322, H2126) established in NU/J nude female mice^[1]
Dosage:

12.5 mg/kg
Administration:

Intraperitoneal injection (i.p.), once daily for 25-26 days
Result:

Showed significant tumor growth inhibition (TGI) of 72% (H1568), 49% (H322), and 44% (H2126).
Effectively degraded SMARCA2 in vivo.
Showed a slight weight loss (<10%), indicating good tolerance.

Chemical Information

CAS. Nr. 2951015-29-3
Appearance Solid
Molecular Weight 738.76
Formel C₃₈H₃₉FN₈O₇
Color Light yellow to yellow
SMILES

O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCOC4=C(F)C=C(CN5CCN(C6=C(N)N=NC(C7=C(O)C=CC=C7)=C6)CC5)C=C4)=O
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 : 100 mg/mL (135.36 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

1.3536 mL

6.7681 mL

13.5362 mL

5 mM

0.2707 mL

1.3536 mL

2.7072 mL

10 mM

0.1354 mL

0.6768 mL

1.3536 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 (272 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]. Kotagiri S, et al. Novel SMARCA2 degrading bifunctional molecules as therapeutics in SMARCA4 mutant lung cancer[J]. Cancer Research, 2023, 83(7_Supplement): 1138-1138.

[2]. Kotagiri S, et al. Enhancer reprogramming by novel SMARCA2 degrading PROTACs underlies therapeutic utility in SMARCA4 mutant tumors[J]. Cancer Research, 2023, 83(7_Supplement): 6289-6289.

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	1.3536 mL	6.7681 mL	13.5362 mL	33.8405 mL
	5 mM	0.2707 mL	1.3536 mL	2.7072 mL	6.7681 mL
	10 mM	0.1354 mL	0.6768 mL	1.3536 mL	3.3840 mL
	15 mM	0.0902 mL	0.4512 mL	0.9024 mL	2.2560 mL
	20 mM	0.0677 mL	0.3384 mL	0.6768 mL	1.6920 mL
	25 mM	0.0541 mL	0.2707 mL	0.5414 mL	1.3536 mL
	30 mM	0.0451 mL	0.2256 mL	0.4512 mL	1.1280 mL
	40 mM	0.0338 mL	0.1692 mL	0.3384 mL	0.8460 mL
	50 mM	0.0271 mL	0.1354 mL	0.2707 mL	0.6768 mL
	60 mM	0.0226 mL	0.1128 mL	0.2256 mL	0.5640 mL
	80 mM	0.0169 mL	0.0846 mL	0.1692 mL	0.4230 mL
	100 mM	0.0135 mL	0.0677 mL	0.1354 mL	0.3384 mL

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

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

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Art. -Nr.:
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YD23

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle SWI/SNF Complex Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YD23

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

PROTAC Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle SWI/SNF Complex Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YD23 Related Classifications

HY-153361 Related Classifications