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PD-1/PD-L1 inhibitor 2

PD-1/PD-L1 interaction inhibitor CAS# 1675203-84-5

PD-1/PD-L1 inhibitor 2

2D Structure

Catalog No. BCC6520----Order now to get a substantial discount!

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PD-1/PD-L1 inhibitor 2: 5mg $115 In Stock
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Quality Control of PD-1/PD-L1 inhibitor 2

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PD-1/PD-L1 inhibitor 2

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Chemical Properties of PD-1/PD-L1 inhibitor 2

Cas No. 1675203-84-5 SDF Download SDF
PubChem ID 117951478 Appearance Powder
Formula C25H29N3O3 M.Wt 419.52
Type of Compound N/A Storage Desiccate at -20°C
Synonyms PD-1/PD-L1 inhibitor 2
Solubility DMSO : ≥ 100 mg/mL (238.37 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[2-[[2-methoxy-6-[(2-methyl-3-phenylphenyl)methoxy]pyridin-3-yl]methylamino]ethyl]acetamide
SMILES CC1=C(C=CC=C1COC2=NC(=C(C=C2)CNCCNC(=O)C)OC)C3=CC=CC=C3
Standard InChIKey JEDPSOYOYVELLZ-UHFFFAOYSA-N
Standard InChI InChI=1S/C25H29N3O3/c1-18-22(10-7-11-23(18)20-8-5-4-6-9-20)17-31-24-13-12-21(25(28-24)30-3)16-26-14-15-27-19(2)29/h4-13,26H,14-17H2,1-3H3,(H,27,29)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PD-1/PD-L1 inhibitor 2

DescriptionBMS-202 is an inhibitor of the PD-1/PD-L1 protein/protein interaction, mainly used for cancer treatment.In Vitro:BMS-202 inhibits PD-1/PD-Ll interaction, and may augment therapeutic immune response to a number of histologically distinct tumors. Blockade of the PD-1/PD-Ll ligation using antibodies to PD-Ll has been shown to restore and augment T cell activation in many systems[1].

References:
[1]. Louis S. Chupak, et al. Compounds useful as immunomodulators. WO 2015034820 A1

Protocol

Kinase Assay [1]
All binding studies are performed in an HTRF assay buffer consisting of dPBS supplemented with 0.1% (with v) bovine serum albumin and 0.05% (v/v) Tween-20. For the PD-l-Ig/PD-Ll-His binding assay, inhibitors are pre-incubated with PD-Ll-His (10 nM final) for 15 m in 4 μL of assay buffer, followed by addition of PD-l-Ig (20 nM final) in 1 μL of assay buffer and further incubation for 15 m. PD-L1 from either human, cyno, or mouse are used. HTRF detection is achieved using europium crypate-labeled anti- Ig (1 nM final) and allophycocyanin (APC) labeled anti-His (20 nM final). Antibodies are diluted in HTRF detection buffer and 5 μL is dispensed on top of binding reaction. The reaction mixture is allowed to equilibrate for 30 minutes and signal (665 nm/620 nm ratio) is obtained using an En Vision fluorometer. Additional binding assays are established between PD-1-Ig/PD-L2-His (20, 5 nM, respectively), CD80-His/PD-Ll-Ig (100, 10 nM, respectively) and CD80-His/CTLA4-Ig (10, 5 nM, respectively).

References:
[1]. Louis S. Chupak, et al. Compounds useful as immunomodulators. WO 2015034820 A1

PD-1/PD-L1 inhibitor 2 Dilution Calculator

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PD-1/PD-L1 inhibitor 2 Molarity Calculator

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Preparing Stock Solutions of PD-1/PD-L1 inhibitor 2

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3837 mL 11.9184 mL 23.8368 mL 47.6735 mL 59.5919 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 mL 9.5347 mL 11.9184 mL
10 mM 0.2384 mL 1.1918 mL 2.3837 mL 4.7674 mL 5.9592 mL
50 mM 0.0477 mL 0.2384 mL 0.4767 mL 0.9535 mL 1.1918 mL
100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.4767 mL 0.5959 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on PD-1/PD-L1 inhibitor 2

PD-1/PD-L1 inhibitor 2 is a PD-1/PD-L1 interaction inhibitor.

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Description

BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.

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