2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. PD-1/PD-L1-IN-9

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.

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PD-1/PD-L1-IN-9 Chemical Structure

PD-1/PD-L1-IN-9 Chemical Structure

CAS No. : 2628506-54-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
5 mg USD 280 In-stock
10 mg USD 420 In-stock
25 mg USD 670 In-stock
50 mg USD 910 In-stock
100 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of PD-1/PD-L1-IN-9:

PD-1/PD-L1-IN-9 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PD-1/PD-L1-IN-9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model[1].

IC50 & Target

IC50: 3.8 nM (PD-1/PD-L1)[1]
Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 EC50
100 nM
Compound: 24
Antitumor immunity against human MDA-MB-231 cells co-cultured with CD3/CD28/CD2 T cell activator stimulated human PMBC assessed as cell death measuring lactate dehydrogenase release measured for 12 hrs by PBMC killing assay
Antitumor immunity against human MDA-MB-231 cells co-cultured with CD3/CD28/CD2 T cell activator stimulated human PMBC assessed as cell death measuring lactate dehydrogenase release measured for 12 hrs by PBMC killing assay
[PMID: 34056906]
In Vitro

PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of peripheral blood mononuclear cells (PBMCs) to MDB-MB 231 cells, with an EC50 of ∼100 nM[1].

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

PD-1/PD-L1-IN-9 Related Antibodies
In Vivo

PD-1/PD-L1-IN-9 (compound 24) (40-80 mg/kg; p.o.; once a day for 2 weeks) inhibits tumor growth in a dose-dependent manner and does not cause any body weight loss or mortality of mice[1].
PD-1/PD-L1-IN-9 (3 mg/kg; i.v.; single dose) exhibits half-life (T1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) and Cmax (1233 ng/mL) in rats[1].
PD-1/PD-L1-IN-9 (25 mg/kg; p.o.; single dose) exhibits moderate oral bioavailability (F=22 %), half-life (t1/2=6.4 h) and Cmax (192 ng/mL) in rats[1].

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

Animal Model: Male BALB/c mice (5-6 weeks) were inoculated CT26 cells[1]
Dosage: 40 mg/kg, 80 mg/kg
Administration: Oral gavage; once daily, for 2 weeks
Result: Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
Animal Model: Pharmacokinetic analysis in sprague-Dawley (SD) rats[1]
Dosage: 3 mg/kg and 25 mg/kg
Administration: Intravenous injection or oral gavage; single dose
Result:
Route Dose (mg/kg) AUC(0-t) (ng·h/mL) Cmax (ng/mL) t1/2 (h) Tmax Cl (L·h/kg) Vz (L/kg) F (%)
i.v. 3 430.5 1233 4.2 0.03 11.5 78.6 /
p.o. 25 787.4 192 6.4 0.69 28.8 249.3 22
Molecular Weight

348.44

Formula

C22H24N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C=CC=C1C2=CC=CC=C2)C3=NC(OC)=C(C=C3)CNCCO
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 (286.99 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 2.8699 mL 14.3497 mL 28.6993 mL
5 mM 0.5740 mL 2.8699 mL 5.7399 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.8699 mL 14.3497 mL 28.6993 mL 71.7484 mL
5 mM 0.5740 mL 2.8699 mL 5.7399 mL 14.3497 mL
10 mM 0.2870 mL 1.4350 mL 2.8699 mL 7.1748 mL
15 mM 0.1913 mL 0.9566 mL 1.9133 mL 4.7832 mL
20 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5874 mL
25 mM 0.1148 mL 0.5740 mL 1.1480 mL 2.8699 mL
30 mM 0.0957 mL 0.4783 mL 0.9566 mL 2.3916 mL
40 mM 0.0717 mL 0.3587 mL 0.7175 mL 1.7937 mL
50 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4350 mL
60 mM 0.0478 mL 0.2392 mL 0.4783 mL 1.1958 mL
80 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.8969 mL
100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7175 mL
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PD-1/PD-L1-IN-9 Related Classifications

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.

Keywords:

PD-1/PD-L1-IN-92628506-54-5PD-1/PD-L1PD-1/Programmed death-ligand 1PD-1PD-L1interactiontumorInhibitorinhibitorinhibit

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