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Chemical Structure| 2230911-59-6 Chemical Structure| 2230911-59-6

Structure of INCB086550
CAS No.: 2230911-59-6

Chemical Structure| 2230911-59-6

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Synonyms: PD-1/PD-L1-IN-8

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Product Details of INCB086550

CAS No. :2230911-59-6
Formula : C41H39N7O4
M.W : 693.79
SMILES Code : O=C([C@H]1CN(CC2=CC(C#N)=C(OC(C3=C(C)C(C4=CC=CC(NC5=C6N=CC(CN7C[C@H](O)CC7)=CC6=CC=N5)=C4C)=CC=C3)=N8)C8=C2)CC1)O
Synonyms :
PD-1/PD-L1-IN-8
MDL No. :MFCD34549780
InChI Key :QARLNMDDSQMINK-BVRKHOPBSA-N
Pubchem ID :135146787

Safety of INCB086550

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

Target
  • PD-1/PD-L1 interaction

    PD-1/PD-L1, IC50:<10 nM

  • PD-1/PD-L1

    PD-1/PD-L1, IC50:<10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-231 cells 1 µmol/L 18 hours To evaluate the effect of INCB086550 on PD-L1 internalization, results showed that INCB086550 significantly reduced cell-surface PD-L1. Cancer Discov. 2022 Jun 2;12(6):1482-1499
CHO PD-L1 cells 13.2 nmol/L (IC50) 1 hour To evaluate the ability of INCB086550 to block the PD-L1/PD-1 interaction, results showed that INCB086550 effectively blocked PD-L1 binding to PD-1. Cancer Discov. 2022 Jun 2;12(6):1482-1499

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice 4T1-hPD-L1 syngeneic mouse model Subcutaneous injection 15 mg/kg INCB086550 (twice daily, BID) INCB086550 treatment for 4 weeks, Deucravacitinib treatment for 2 weeks To evaluate the antitumor effect of INCB086550 in combination with Deucravacitinib in the 4T1-hPD-L1 model. Results showed that the combination therapy significantly reduced tumor volume and weight, increased the proportion of T cells, B cells, and NK cells, and decreased the proportion of MDSCs. Anticancer Drugs. 2025 Apr 1;36(4):280-289
Mice MC38 huPD-L1 tumor model Oral 2, 20, 200 mg/kg Twice daily for 14 days To evaluate the antitumor efficacy of INCB086550 in vivo, results showed that INCB086550 significantly inhibited tumor growth and increased CD8+ T-cell infiltration. Cancer Discov. 2022 Jun 2;12(6):1482-1499
BALB/c mice 4T1-hPD-L1 syngeneic mouse model Oral 15 mg/kg INCB086550 (twice daily) and 20 mg/kg Deucravacitinib (twice daily) INCB086550 treatment for 4 weeks, Deucravacitinib treatment for 2 weeks To verify the antitumor efficacy of INCB086550 combined with Deucravacitinib in triple-negative breast cancer models. Results showed that the combination therapy significantly reduced tumor volume and weight, increased the counts of T, B, and natural killer cells, and decreased the proportion of myeloid-derived suppressor cells. Anticancer Drugs. 2025 Apr 1;36(4):280-289

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04629339 Non Small Cell Lung Cancer|Uro... More >>thelial Cancer|Renal Cell Carcinoma|Hepatocellular Carcinoma|Melanoma Less << PHASE2 TERMINATED 2024-03-26 Complex Oncology Center - Burg... More >>as Eood, Burgas, 8000, Bulgaria|Multiprofile Hospital For Active Treatment "Dr. Tota Venkova" Jsc, Gabrovo, 5300, Bulgaria|Complex Onclogy Center Plovdiv Eood, Plovdiv, 4004, Bulgaria|Shatod Dr. Marko - Varna Ltd, Varna, 9000, Bulgaria|Semmelweis Egyetem, Budapest, 1085, Hungary|Complex Oncology Center - Burgas Eood, Farkasgyepu, 8582, Hungary|Bacs Kiskun Megyei Oktatokorhaz, Kecskemet, 6000, Hungary|The Catholic University of Korea St. Vincent'S Hospital, Gyeonggi-do, 16427, Korea, Republic of|Korea University Anam Hospital, Seoul, 02841, Korea, Republic of|Severance Hospital Yonsei University Health System, Seoul, 03722, Korea, Republic of|Asan Medical Center, Seoul, 05505, Korea, Republic of|Ajou University Hospital, Suwon, 16499, Korea, Republic of|Chang Gung Memorial Hospital Linkou, Taoyuan City, 33305, Taiwan|Multifield Clinical Hospital No 4, Dnipro, 49102, Ukraine|Ci of Healthcare Regional Clinical Specialized Dispensary of the Radiation Protection, Kharkiv, 61166, Ukraine|Mi Kryviy Rih Center of Dnipropetrovsk Regional Council, Kryvyi Rih, 50048, Ukraine|Volyn Regional Oncological Dispensary, Lutsk, 43018, Ukraine|Rmi Sumy Regional Clinical Oncology Dispensary, Sumy, 40022, Ukraine|Cne Ccch of Uzh Cc Oncological Center, Uzhgorod, 88000, Ukraine|Medical Clinic Innovacia Llc, Vyshhorod, 07352, Ukraine Less <<
NCT05101369 Healthy Volunteers PHASE1 COMPLETED 2022-03-25 Covance Leeds Cru, Leeds, LS2 ... More >>9LH, United Kingdom Less <<
NCT03762447 Solid Tumors PHASE1 COMPLETED 2023-11-17 Georgetown University Hospital... More >>, Washington, District of Columbia, 20007, United States|H. Lee Moffitt Cancer Center and Research Institute Hospital, Tampa, Florida, 33612, United States|Aamc Oncology and Hematology, Annapolis, Maryland, 21401, United States|University of Pennsylvania Health System, Philadelphia, Pennsylvania, 19104, United States|Jefferson University Hospitals, Philadelphia, Pennsylvania, 19107, United States|Sarah Cannon Research Institute, Nashville, Tennessee, 37203, United States|Md Anderson Cancer Center, Houston, Texas, 77030, United States|Institut Jules Bordet, Brussels, 01000, Belgium|Universitair Ziekenhuis Antwerpen (Uza), Edegem, 02650, Belgium|Universitair Ziekenhuis Gent, Gent, 09000, Belgium|Universitaire Ziekenhuis Leuven - Gasthuisberg, Leuven, 03000, Belgium|Chu Hopital de La Timone, Marseille Cedex 5, 13385, France|Icm Montpellier, Montpellier Cedex 5, 34298, France|Institut Curie, Paris, 75005, France|Institut Universitaire Du Cancer de Toulouse Oncopole, Toulouse, 31059, France|Fondazione Irccs Istituto Nazionale Dei Tumori, Milan, 20133, Italy|European Institute of Oncology, Milan, 20141, Italy|Istituto Nazionale Tumori Irccs Fondazione Pascale, Napoli, 80131, Italy|Irrcs Instituto Clinico Humanitas, Rozzano, 20089, Italy|Azienda Ospedaliera Universitaria Senese Policlinico Santa Maria Alle Scotte, Siena, 53100, Italy|Addenbrooke'S Hospital, Cambridge, CB2 0QQ, United Kingdom|Guys and St Thomas Nhs Foundation Trust, London, SE1 9RT, United Kingdom|Imperial College Healthcare Nhs Trust - Hammersmith Hospital, London, W12 0HS, United Kingdom|The Christie Nhs Foundation Trust Uk, Manchester, M20 4BX, United Kingdom|Weston Park Hospital, Sheffield, S10 2SJ, United Kingdom Less <<
NCT04674748 Solid Tumors PHASE1 TERMINATED 2022-05-13 National Cancer Center Hospita... More >>l - East, Chiba, 277-8577, Japan|National Cancer Center Hospital, Tokyo, 104-0045, Japan Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.44mL

0.29mL

0.14mL

7.21mL

1.44mL

0.72mL

14.41mL

2.88mL

1.44mL

 

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