1. PROTAC Immunology/Inflammation
  2. PROTACs PD-1/PD-L1
  3. PROTAC PD-L1 degrader-2

PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC50 of 197.4 nM and exhibits an affinity with PD-L1 with a Kd of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model.

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PROTAC PD-L1 degrader-2

PROTAC PD-L1 degrader-2 Chemical Structure

CAS No. : 2995357-09-8

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Description

PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC50 of 197.4 nM and exhibits an affinity with PD-L1 with a Kd of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model[1].

Molecular Weight

861.31

Formula

C46H42ClFN6O8

CAS No.
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
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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  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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 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
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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.

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Product Name:
PROTAC PD-L1 degrader-2
Cat. No.:
HY-162972
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