PROTAC PD-L1 degrader-2

Name: PROTAC PD-L1 degrader-2
Brand: MedChemExpress
SKU: HY-162972
Rating: 4.5 (0 reviews)

Cat. No.: HY-162972 Purity: 95.23%: Data Sheet
COA

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PROTAC PD-L1 degrader-2 is a PD-L1 PROTAC degrader with an IC₅₀ of 197.4 nM and a K_d of 301 nM. PROTAC PD-L1 degrader-2 induces PD-L1 endocytosis, drives degradation via the proteasomal and lysosomal pathways, and inhibits the PD-1/PD-L1 interaction. As an immune activator, PROTAC PD-L1 degrader-2 increases the levels of CD4⁺, CD8⁺, granzyme B and perforin. PROTAC PD-L1 degrader-2 can be used in studies related to colon cancer immunology.
(Pink: PD-1/PD-L1 ligand (HY-162973); Blue: Cereblon ligand (HY-W867704); Black: linker (HY-128833)).

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

PROTAC PD-L1 degrader-2 Chemical Structure

CAS No. : 2995357-09-8

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	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Purity & Documentation
References
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Description

PROTAC PD-L1 degrader-2 is a PD-L1 PROTAC degrader with an IC₅₀ of 197.4 nM and a K_d of 301 nM. PROTAC PD-L1 degrader-2 induces PD-L1 endocytosis, drives degradation via the proteasomal and lysosomal pathways, and inhibits the PD-1/PD-L1 interaction. As an immune activator, PROTAC PD-L1 degrader-2 increases the levels of CD4⁺, CD8⁺, granzyme B and perforin. PROTAC PD-L1 degrader-2 can be used in studies related to colon cancer immunology^[1]. (Pink: PD-1/PD-L1 ligand (HY-162973); Blue: Cereblon ligand (HY-W867704); Black: linker (HY-128833)).

In Vitro

PROTAC PD-L1 degrader-2 (Compound 9i) (1.25-20 μM; 24 h) induces concentration-dependent degradation of PD-L1 in HCC-827 cells, with a degradation rate of 60.87% after treatment at 20 μM for 24 h^[1].
PROTAC PD-L1 degrader-2 (0.25-10 μM; 24 h) induces concentration-dependent degradation of PD-L1 in SK-N-AS, 786-O and MC38 cells, exhibiting broad-spectrum PD-L1 degradation activity^[1].
PROTAC PD-L1 degrader-2 (1.25-10 μM; 24 h) enhances T cell-mediated killing of HCC-827 cells in a co-culture model, reduces the survival rate of HCC-827 cells to 50.65% after treatment at 10 μM for 24 h, and exhibits low cytotoxicity against Jurkat cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	human non-small cell lung cancer HCC-827 cells
Concentration:	1.25, 2.5, 5, 10 and 20 μM
Incubation Time:	24 h
Result:	Induced concentration-dependent degradation of PD-L1 in HCC-827 cells. Achieved a 60.87% degradation rate at 20 μM after 24 h.

Western Blot Analysis^[1]

Cell Line:	human neuroblastoma SK-N-AS cells, human renal carcinoma 786-O cells, mouse colon cancer MC38 cells
Concentration:	0.25, 1.25, 2.5, 5 and 10 μM
Incubation Time:	24 h
Result:	Induced concentration-dependent degradation of PD-L1 in all three cell lines. Reduced PD-L1 levels significantly in SK-N-AS cells at concentrations ≥ 1.25 μM. Reduced PD-L1 levels significantly in 786-O cells at concentrations ≥ 2.5 μM. Reduced PD-L1 levels significantly in MC38 cells at 10 μM.

Cell Cytotoxicity Assay^[1]

Cell Line:	HCC-827/Jurkat cell co-culture model
Concentration:	1.25, 2.5, 5, 10 and 20 μM
Incubation Time:	24 h
Result:	Reduced HCC-827 cell survival rate to 50.65% at 10 μM in the co-culture system, indicating enhanced Jurkat-mediated tumor cell killing. Showed negligible toxicity to Jurkat cells at concentrations ≤ 10 μM.

In Vivo

PROTAC PD-L1 degrader-2 (Compound 9i) (10-20 mg/kg; i.p.; daily; 15 days) delivers dose-dependent antitumor activity in a mouse MC38 colon cancer model^[1].

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

Animal Model:	C57BL/6 (female, 6 weeks old, 18-22 g, subcutaneous inoculation of MC38 colon cancer cells)^[1]
Dosage:	10 mg/kg; 20 mg/kg
Administration:	i.p.; daily; 15 days
Result:	Achieved a tumor growth inhibition (TGI) rate of 48.72% at 10 mg/kg. Achieved a tumor growth inhibition (TGI) rate of 57.35% at 20 mg/kg. Significantly downregulated PD-L1 protein levels in tumor tissues. Increased mRNA expression of immune chemokines CXCR3, CXCL9, and CXCL10. Elevated the CD8⁺/CD4⁺ T cell ratio in lymph nodes and tumor tissue. Increased granzyme B and perforin expression in tumor tissues. Caused no significant changes in body weight, organ histology (H&E staining), or blood parameters, indicating no obvious toxicity.

Molecular Weight

861.31

Formula

C₄₆H₄₂ClFN₆O₈

CAS No.

2995357-09-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=C(C=CC=C1C2=CC=CC=C2F)COC3=CC(OCC4=CC(C#N)=CN=C4)=C(C=C3)CNCCOCCOCCNC5=C(C6=CC=C5)C(N(C6=O)C7C(NC(CC7)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (116.10 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	1.1610 mL	5.8051 mL	11.6102 mL
5 mM	0.2322 mL	1.1610 mL	2.3220 mL
10 mM	0.1161 mL	0.5805 mL	1.1610 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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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 95.23%

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Data Sheet (275 KB) SDS (252 KB)

COA (245 KB) HNMR (276 KB) RP-HPLC (263 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang F, et al., Design, synthesis, anti-tumor activity and mechanism of novel PROTACs as degraders of PD-L1 and inhibitors of PD-1/PD-L1 interaction. Bioorg Med Chem. 2024 Sep 1;111:117867.
[Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.1610 mL	5.8051 mL	11.6102 mL	29.0256 mL
	5 mM	0.2322 mL	1.1610 mL	2.3220 mL	5.8051 mL
	10 mM	0.1161 mL	0.5805 mL	1.1610 mL	2.9026 mL
	15 mM	0.0774 mL	0.3870 mL	0.7740 mL	1.9350 mL
	20 mM	0.0581 mL	0.2903 mL	0.5805 mL	1.4513 mL
	25 mM	0.0464 mL	0.2322 mL	0.4644 mL	1.1610 mL
	30 mM	0.0387 mL	0.1935 mL	0.3870 mL	0.9675 mL
	40 mM	0.0290 mL	0.1451 mL	0.2903 mL	0.7256 mL
	50 mM	0.0232 mL	0.1161 mL	0.2322 mL	0.5805 mL
	60 mM	0.0194 mL	0.0968 mL	0.1935 mL	0.4838 mL
	80 mM	0.0145 mL	0.0726 mL	0.1451 mL	0.3628 mL
	100 mM	0.0116 mL	0.0581 mL	0.1161 mL	0.2903 mL