PD-1/PD-L1-IN-10

Name: PD-1/PD-L1-IN-10
Brand: MedChemExpress
SKU: HY-132202
Rating: 4.5 (1 reviews)

Cat. No.: HY-132202 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC₅₀ of 2.7 nM) with potent anticancer efficacy.

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

PD-1/PD-L1-IN-10 Chemical Structure

CAS No. : 2487550-41-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 143	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 143	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1150	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC₅₀ of 2.7 nM) with potent anticancer efficacy^[1].

IC₅₀ & Target

IC50: 2.7 nM (PD-1/PD-L1)^[1].

In Vitro

PD-1/PD-L1-IN-10 (compound B2) significantly promotes interferongamma secretion in a dose-dependent manner in vitro even at the low concentration of 1 nM^[1].
PD-1/PD-L1-IN-10 (compound B2) does not affect cell viability of LLC cells and lymph node T-cells^[1].
PD-1/PD-L1-IN-10 (compound B2, 0-100 nM) stabilizes the PD-L1 protein in mouse Lewis lung carcinoma (LLC) cells. In particular, PD-1/PD-L1-IN-10 (compound B2) maintains the PD-L1 stability in a dose-dependent manner at 58 °C. Suggesting that PD-1/PD-L1-IN-10 (compound B2) could enter LLC cells and then directly binds to the PD-L1 protein^[1].

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

In Vivo

PD-1/PD-L1-IN-10 (compound B2, 5 mg/kg, intragastric gavage) exhibits potent in vivo anticancer efficacy in an LLC-bearing allograft mouse model. PD-1/PD-L1-IN-10 (compound B2) effectively blocks tumor cell proliferation and induces apoptosis in LLC tumor tissues.^[1].

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

Animal Model:	LLC tumor-bearing mice^[1].
Dosage:	2, 5 mg/kg.
Administration:	i.g., qd., for 21 days
Result:	Significantly suppressed the growth of the tumor in a dose-dependent manner compared with the vehicle group.

Molecular Weight

581.62

Formula

C₃₃H₃₁N₃O₇

CAS No.

2487550-41-2

Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C=CC=C1C2=CC=CC=C2)COC3=C(C=C(C(OCC4=CC(C#N)=CC=C4)=C3)CN[C@H](C(O)=O)C(O)C)[N+]([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 (171.93 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	1.7193 mL	8.5967 mL	17.1934 mL
5 mM	0.3439 mL	1.7193 mL	3.4387 mL
10 mM	0.1719 mL	0.8597 mL	1.7193 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.30 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)

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

Purity: 99.61%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (253 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Yiqiang OuYang, et al. Design, Synthesis, and Evaluation of o-(Biphenyl-3-ylmethoxy)nitrophenyl Derivatives as PD-1/PD-L1 Inhibitors with Potent Anticancer Efficacy In Vivo. J Med Chem. 2021 May 26. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7193 mL	8.5967 mL	17.1934 mL	42.9834 mL
	5 mM	0.3439 mL	1.7193 mL	3.4387 mL	8.5967 mL
	10 mM	0.1719 mL	0.8597 mL	1.7193 mL	4.2983 mL
	15 mM	0.1146 mL	0.5731 mL	1.1462 mL	2.8656 mL
	20 mM	0.0860 mL	0.4298 mL	0.8597 mL	2.1492 mL
	25 mM	0.0688 mL	0.3439 mL	0.6877 mL	1.7193 mL
	30 mM	0.0573 mL	0.2866 mL	0.5731 mL	1.4328 mL
	40 mM	0.0430 mL	0.2149 mL	0.4298 mL	1.0746 mL
	50 mM	0.0344 mL	0.1719 mL	0.3439 mL	0.8597 mL
	60 mM	0.0287 mL	0.1433 mL	0.2866 mL	0.7164 mL
	80 mM	0.0215 mL	0.1075 mL	0.2149 mL	0.5373 mL
	100 mM	0.0172 mL	0.0860 mL	0.1719 mL	0.4298 mL

PD-1/PD-L1-IN-10 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-102487550-41-2PD-1/PD-L1ApoptosisPD-1/Programmed death-ligand 1LewislungcarcinomaLLCtumorT-lymphocyteIFN-γ,Inhibitorinhibitorinhibit

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PD-1/PD-L1-IN-10

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Complete Stock Solution Preparation Table

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