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Pembrolizumab (anti-PD-1)

规格或纯度: Purity>95% (SDS-PAGE&SEC); Endotoxin Level<1.0EU/mg; Human IgG4SP; CHO; ELISA, FACS, Functional assay, Animal Model; Unconjugated
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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
P411997-1mg 1mg 现货 Stock Image
P411997-5mg 5mg 现货 Stock Image
P411997-10mg 10mg 期货 Stock Image

基本描述

规格或纯度 Purity>95% (SDS-PAGE&SEC); Endotoxin Level<1.0EU/mg; Human IgG4SP; CHO; ELISA, FACS, Functional assay, Animal Model; Unconjugated
英文名称 Pembrolizumab (anti-PD-1)
别名 派姆单抗; 帕博利珠单抗; Recombinant Pembrolizumab Antibody; Pembrolizumab (anti-PD-1); Pembrolizumab; MK-3475; Lambrolizumab; CD279 antibody; CD279 antigen antibody; hPD 1 antibody; hPD l antibody; hPD-1 antibody; hSLE1 antibody; PD 1 antibody; PD-1 antibody; PD1 a
英文别名 Recombinant Pembrolizumab Antibody; Pembrolizumab (anti-PD-1); Pembrolizumab; MK-3475; Lambrolizumab; CD279 antibody; CD279 antigen antibody; hPD 1 antibody; hPD l antibody; hPD-1 antibody; hSLE1 antibody; PD 1 antibody; PD-1 antibody; PD1 antibody; PDCD
应用 ELISA,Functional Assay,Flow cytometry,Kinetics (BLI),Kinetics (SPR)
来源 CHO supernatant
储存温度 -80℃储存,避免反复冻融
运输条件 超低温冰袋运输
产品介绍

Pembrolizumab 是一种有效的、高选择性的、人源IgG4-kappa单克隆抗体,同时也是抑制剂,靶向PD-1,具有潜在的免疫检查点抑制活性和抗肿瘤活性。

Pembrolizumab (anti-PD-1) is a potent, highly selective, fully humanized immunoglobulin (Ig) G4-kappa monoclonal antibody against PD-1 with potential immune checkpoint inhibitory and antineoplastic activities.
Purity
>95% (SDS-PAGE&SEC)
Endotoxin Level
< 1.0EU/mg?

名称和标识符

EC号 807-012-2
IUPAC Name 1-butyl-4-propylpiperazine;ethane;1-[hex-5-enyl(2-methyltetradecyl)amino]tetradecan-2-ol;3-[2-methylhexadeca-8,10-dienyl(2-methylhexadeca-9,11-dienyl)amino]propane-1-thiol
INCHI InChI=1S/C37H69NS.C35H71NO.C11H24N2.C2H6/c1-5-7-9-11-13-15-17-19-21-23-25-27-30-36(3)34-38(32-29-33-39)35-37(4)31-28-26-24-22-20-18-16-14-12-10-8-6-2;1-5-8-11-14-16-18-20-22-24-26-29-34(4)32-36(31-28-13-10-7-3)33-35(37)30-27-25-23-21-19-17-15-12-9-6-2;1-3-5-7-13-10-8-12(6-4-2)9-11-13;1-2/h11,13-18,20,36-37,39H,5-10,12,19,21-35H2,1-4H3;7,34-35,37H,3,5-6,8-33H2,1-2,4H3;3-11H2,1-2H3;1-2H3
InChi Key AMOIBCKFWIUEKF-UHFFFAOYSA-N
Canonical SMILES CC.CCCCCCCCCCCCC(C)CN(CCCCC=C)CC(CCCCCCCCCCCC)O.CCCCCC=CC=CCCCCCC(C)CN(CCCS)CC(C)CCCCCCC=CC=CCCCC.CCCCN1CCN(CC1)CCC
关联CAS 1374853-91-4
PubChem CID 168009853

化学和物理性质

稳定性与储存 Store at -80℃ for 18 months. Upon delivery aliquot. Avoid freeze/thaw cycle.

靶标

Target ID 2760
名称 programmed cell death 1 (CD279)
缩写名 PD-1
家族 Other immune checkpoint proteins
别名 KCa2.1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 288 2q37.3 PDCD1 programmed cell death 1
Mouse 1 288 1 D Pdcd1 programmed cell death 1
Rat 1 287 9q36 Pdcd1 programmed cell death 1
OMIM 600244 (Hs)
UniProtKB Q15116 (Hs) , Q02242 (Mm)
Ensembl Gene ENSG00000188389 (Hs) , ENSMUSG00000026285 (Mm) , ENSRNOG00000019043 (Rn)
RefSeq Nucleotide NM_005018 (Hs) , NM_001106927 (Rn) , NM_008798 (Mm)
RefSeq Protein NP_005009 (Hs) , NP_001100397 (Rn) , NP_032824 (Mm)
Entrez Gene 5133 (Hs) , 301626 (Rn) , 18566 (Mm)
Protein GI 167857792 (Hs) , 6679239 (Mm) , 157817590 (Rn)
CATH/Gene3D 2.60.40.10 (N/A)
ChEMBL Target CHEMBL3307223 (Hs) , CHEMBL4630756 (Mm)

关联配体

Ligand ID 7499
名称 pembrolizumab
别名 lambrolizumab
类别 Antibody
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Pembrolizumab is the first-in-class, anti-PD-1 antibody to be approved by the US FDA.
Full peptide sequence and disulphide bond information is available from the IMGT/mAb-DB entry for this antibody.

Pembrolizumab is the first immuno-oncology therapeutic to be approved for use in cancers of any tissue type, so long as they express a specific genetic biomarker (i.e. high microsatellite instability (MSI-H) or mismatch repair deficient (dMMR) tumours). This is an important breakthrough, since up until this point FDA approvals, including earlier approvals for pembrolizumab, had always been restricted to certain tissue-specific cancers.
配体家族 Immune checkpoint modulators
单字母多肽序列
三字母多肽序列
翻译后修饰
化学修饰
临床描述 The present study has 5 parts. In Parts A and A1, the dose of intravenous (IV) pembrolizumab (MK-3475) will be escalated from 1 to 10 mg/kg to determine the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D) for participants with a histologically- or cytologically-confirmed diagnosis of any type of carcinoma or melanoma (MEL) by evaluating the Dose Limiting Toxicities (DLTs). Following completion of the dose escalation, additional patients will be enrolled in Part A2 to further define pharmacokinetic characteristics. Part B of the study will investigate the safety, tolerability, and efficacy of pembrolizumab (2 mg/kg and 10 mg/kg) in participants with advanced or metastatic MEL and compare every 2 week dosing (Q2W) to every 3 week dosing (Q3W). Part C of the study will investigate the safety, tolerability, and efficacy of pembrolizumab administered at 10 mg/kg Q3W in participants with non-small cell lung carcinoma (NSCLC) that is locally advanced or metastatic. Part D of the study will investigate the low and high doses of study drug identified in Parts A and B (2 mg/kg and 10 mg/kg) administered Q3W in participants with advanced or metastatic MEL. Part E (closed with Amendment 7) was planned to investigate low, medium, and high doses of pembrolizumab in combination with standard chemotherapy in participants with locally advanced or metastatic NSCLC. Part F will investigate low and high doses of pembrolizumab (2 mg/kg and 10 mg/kg) administered Q2W or Q3W in treatment-naive and previously-treated participants with NSCLC with programmed cell death 1 ligand (PD-L1) gene expression. The primary hypotheses are the following: that pembrolizumab will have acceptable safety and tolerability; that pembrolizumab will show a clinically meaningful response rate (RR) or disease-control rate (DCR) in participants with melanoma (ipilimumab-refractory or not) and NSCLC, and that pembrolizumab will show a more clinically meaningful RR in participants with either cancer whose tumors express PD-L1.
This phase II trial studies how well pembrolizumab works in treating patients with Merkel cell cancer that cannot be removed by surgery or controlled with treatment, or has spread to other parts of the body. Pembrolizumab may stimulate the immune system to identify and destroy cancer cells.
Participants with recurrent or metastatic (R/M) squamous cell cancer of the head and neck (HNSCC) will be randomly assigned to receive pembrolizumab monotherapy [pembro mono], pembrolizumab plus chemotherapy with a platinum-based drug (cisplatin or carboplatin) and 5-Fluorouracil (5-FU) [pembro combo], or cetuximab plus a platinum-based drug (cisplatin or carboplatin) and 5-FU [control]. The overall primary study hypotheses are as follows in all participants and in participants with Programmed Cell Death Ligand 1 (PD-L1) positive expression defined by Combined Positive Score (CPS) ≥1 and CPS ≥20: 1) pembrolizumab monotherapy prolongs progression free survival (PFS) per Response Evaluation Criteria in Solid Tumors Version 1.1 (RECIST 1.1) assessed by Blinded Independent Central Review (BICR) and prolongs overall survival (OS) compared to standard treatment, and 2) pembrolizumab combination with chemotherapy prolongs PFS per RECIST 1.1 assessed by BICR and prolongs OS compared to standard treatment.
In this study, participants with advanced or metastatic adenocarcinoma or squamous cell carcinoma of the esophagus or Siewert type I adenocarcinoma of the esophagogastric junction (EGJ) that had progressed after first-line standard therapy were randomized to receive either pembrolizumab (MK-3475) OR the Investigator's choice of standard chemotherapy with paclitaxel, docetaxel, or irinotecan. The primary study hypothesis was that treatment with pembrolizumab would prolong overall survival (OS) as compared to treatment with standard chemotherapy.
In this study, participants with relapsed or refractory primary mediastinal large B-cell lymphoma (rrPMBCL) or relapsed or refractory Richter Syndrome (rrRS) will receive pembrolizumab (MK-3475). The efficacy of pembrolizumab in the treatment of rrPMBCL and rrRS will be evaluated. The primary study hypothesis is that intravenous (IV) administration of single agent pembrolizumab will result in an Objective Response Rate (ORR) of greater than 15% using the International Working Group (IWG) response criteria (Cheson, 2007) by independent central review. Effective with Protocol Amendment 04, enrollment into the rrRS cohort was closed.
In this study, participants with multiple types of advanced (unresectable and/or metastatic) solid tumors who have progressed on standard of care therapy will be treated with pembrolizumab (MK-3475).
This is a study of carboplatin and paclitaxel or nano particle albumin-bound paclitaxel (nab-paclitaxel) with or without pembrolizumab (MK-3475, KEYTRUDA?) in adults with first line metastatic squamous non-small cell lung cancer (NSCLC). The primary hypotheses are that treatment with pembrolizumab prolongs: 1) Progression-free Survival (PFS) by Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST 1.1) as assessed by a blinded central imaging vendor compared to placebo, and 2) Overall Survival (OS). After analysis of interim results was conducted, the protocol was amended (Amendment 5) to allow participants the option to discontinue placebo in the control arm and to switch to pembrolizumab in the event of documented progressive disease as assessed by central review.
The purpose of this study is to evaluate the efficacy and safety of pembrolizumab (MK-3475) in combination with axitinib versus sunitinib monotherapy as a first-line treatment for participants with advanced/metastatic renal cell carcinoma (mRCC). The primary hypotheses of this study are: 1. The combination therapy of pembrolizumab plus axitinib is superior to sunitinib monotherapy with respect to Progression-Free Survival (PFS) as assessed by blinded independent central imaging review per Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST 1.1) 2. The combination therapy of pembrolizumab plus axitinib is superior to sunitinib monotherapy with respect to Overall Survival (OS).
This is a study of pembrolizumab plus gemcitabine/cisplatin versus placebo plus gemcitabine/cisplatin as first-line therapy in participants with advanced and/or unresectable biliary tract carcinoma. The primary hypothesis is pembrolizumab plus gemcitabine/cisplatin is superior to placebo plus gemcitabine/cisplatin with respect to overall survival (OS).
来源公司 Merck Sharp & Dohme Corp.
National Cancer Institute (NCI)
Merck Sharp & Dohme Corp.
Merck Sharp & Dohme Corp.
Merck Sharp & Dohme Corp.
Merck Sharp & Dohme Corp.
Merck Sharp & Dohme Corp.
Merck Sharp & Dohme Corp.
Merck Sharp & Dohme LLC

参考文献

1. Janakiram M, Abadi YM, Sparano JA, Zang X.  (2012)  T cell coinhibition and immunotherapy in human breast cancer..  Discov Med,  14  (77):  (229-36).  [PMID:23114578]
2. Greaves P, Gribben JG.  (2013)  The role of B7 family molecules in hematologic malignancy..  Blood,  121  (5):  (734-44).  [PMID:23223433]
3. Tang PA, Heng DY.  (2013)  Programmed death 1 pathway inhibition in metastatic renal cell cancer and prostate cancer..  Curr Oncol Rep,  15  (2):  (98-104).  [PMID:23263823]
4. Hamid O, Robert C, Daud A, Hodi FS, Hwu WJ, Kefford R, Wolchok JD, Hersey P, Joseph RW, Weber JS et al..  (2013)  Safety and tumor responses with lambrolizumab (anti-PD-1) in melanoma..  N Engl J Med,  369  (2):  (134-44).  [PMID:23724846]
5. Nghiem PT, Bhatia S, Lipson EJ, Kudchadkar RR, Miller NJ, Annamalai L, Berry S, Chartash EK, Daud A, Fling SP et al..  (2016)  PD-1 Blockade with Pembrolizumab in Advanced Merkel-Cell Carcinoma..  N Engl J Med,  374  (26):  (2542-52).  [PMID:27093365]
6. Paz-Ares L, Luft A, Vicente D, Tafreshi A, Gümü? M, Mazières J, Hermes B, ?ay ?enler F, Cs?szi T, Fül?p A et al..  (2018)  Pembrolizumab plus Chemotherapy for Squamous Non-Small-Cell Lung Cancer..  N Engl J Med,  379  (21):  (2040-2051).  [PMID:30280635]
7. Rini BI, Plimack ER, Stus V, Gafanov R, Hawkins R, Nosov D, Pouliot F, Alekseev B, Soulières D, Melichar B et al..  (2019)  Pembrolizumab plus Axitinib versus Sunitinib for Advanced Renal-Cell Carcinoma..  N Engl J Med,  380  (12):  (1116-1127).  [PMID:30779529]
8. Saada-Bouzid E, Peyrade F, Guigay J.  (2019)  Immunotherapy in recurrent and or metastatic squamous cell carcinoma of the head and neck..  Curr Opin Oncol,  31  (3):  (146-151).  [PMID:30893146]

图片

Pembrolizumab (anti-PD-1) (P411997) - Flow Cytometry
Flow Cytometry analysis of PHA-stimulated (3 days) human peripheral blood mononuclear lymphocytes labelling PD-1 (red) with Pembrolizumab (anti-PD-1) (P411997). Goat Anti-Human IgG (PE) (Ab175838) at a dilution of 1/1000 was used as the secondary antibody. Blue - Isotype control, human IgG (Ab170213). Black - Unlabelled control, cells without incubation with primary antibody.

Pembrolizumab (anti-PD-1) (P411997) - SEC
The purity of Pembrolizumab (anti-PD-1) (P411997) is more than 95% verified by HPLC.

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