TIM3（CD366；HAVCR2）是一類T細(xì)胞表面抑制性分子，能夠引起癌癥與慢性病毒感染過程中T細(xì)胞的衰竭。與CTLA?4、PD?1類似，TIM3也是目前研究最多的免疫治療靶點之一。TIM家族由TIM1-TIM8八個成員組成，其中TIM1、TIM3和TIM4在人類中發(fā)現(xiàn)。TIM-3由胞外區(qū)、跨膜區(qū)和胞內(nèi)區(qū)三部分構(gòu)成，其中胞外區(qū)由具有FG-CC’環(huán)和N-連接聚糖的N-末端細(xì)胞外免疫球蛋白可變區(qū)（IgV結(jié)構(gòu)域）、含有O-連接糖基化位點的粘蛋白結(jié)構(gòu)域和含有N-連接聚糖的柄結(jié)構(gòu)域組成，跨膜區(qū)由跨膜區(qū)組成，胞內(nèi)區(qū)由帶有五個酪氨酸殘基的胞質(zhì)尾組成。IgV結(jié)構(gòu)域包含其配體的結(jié)合位點。磷脂酰絲氨酸(Ptdser)、癌胚抗原相關(guān)細(xì)胞粘附分子(CEACAM1)和高遷移率族蛋白1 (HMGB1)結(jié)合到FG-CC’環(huán)，而Gal9結(jié)合到N-連接的聚糖。大量證據(jù)表明，TIM基因家族在自身免疫性疾病、感染性疾病、腫瘤免疫監(jiān)視和免疫逃逸等免疫反應(yīng)的調(diào)節(jié)中發(fā)揮著不同的作用。TIM3選擇性地表達(dá)在分泌IFN-γ的T輔助細(xì)胞(Th1和Th17) 、T調(diào)控細(xì)胞(Treg) 、樹突狀細(xì)胞(DCs) 、單核細(xì)胞、肥大細(xì)胞、NK細(xì)胞、腫瘤浸潤性淋巴細(xì)胞(TILs) 上，在腫瘤細(xì)胞上亦有表達(dá)，如黑色素瘤、胃癌、B細(xì)胞淋巴瘤。

貨號：DHJ28402
產(chǎn)品鏈接：http://www.atagenix.com/product_detail-75240.html
產(chǎn)品購買聯(lián)系方式：027-65279366
產(chǎn)品介紹：Sabatolimab (MBG453)是一種高親和力的人源化IgG4 (S228P)抗體，靶向TIM-3，一種調(diào)節(jié)適應(yīng)性和先天免疫反應(yīng)的抑制性受體。Sabatolimab是一種潛在的免疫抑制活性分子，可以靶向免疫細(xì)胞和骨髓細(xì)胞上的TIM-3。
通用名：Sabatolimab
純度：>95% by SDS-PAGE.
濃度：1mg/ml
Formulationicon：0.01M PBS, pH 7.4.
內(nèi)毒素：Please contact with the lab for this information.
別名：MBG-453
靶點;物種：Human CD366/HAVCR2/TIM-3
種類：Humanized
受體鑒定：IgG4-kappa
CAS: 2252262-24-9
存儲條件：Use a manual defrost freezer and avoid repeated freeze-thaw cycles.Store at +4°C short term (1-2 weeks).Store at -20 °C 12 months. Store at -80°C long term.
參考文獻(xiàn)：
Phase I/Ib Clinical Trial of Sabatolimab, an Anti-TIM-3 Antibody, Alone and in Combination with Spartalizumab, an Anti-PD-1 Antibody, in Advanced Solid Tumors. PMID: 33883177
Advances in myelodysplastic syndrome. PMID: 34474438
Characterization of sabatolimab, a novel immunotherapy with immuno-myeloid activity directed against TIM-3 receptor. PMID: 36196369
Immune Checkpoint Inhibition in Acute Myeloid Leukemia and Myelodysplastic Syndromes. PMID: 35883692
Updates on the Management of Acute Myeloid Leukemia. PMID: 36230677
Sabatolimab (MBG453) model-informed drug development for dose selection in patients with myelodysplastic syndrome/acute myeloid leukemia and solid tumors. PMID: 37186155
New Frontiers in Monoclonal Antibodies for the Targeted Therapy of Acute Myeloid Leukemia and Myelodysplastic Syndromes. PMID: 35886899
STIMULUS-MDS2 design and rationale: a phase III trial with the anti-TIM-3 sabatolimab (MBG453) + azacitidine in higher risk MDS and CMML-2. PMID: 37083373
TIM-3: a tumor-associated antigen beyond checkpoint inhibition? PMID: 36406467
Correction to: Characterization of sabatolimab, a novel immunotherapy with immuno-myeloid activity directed against TIM-3 receptor. PMID: 36819977
[Management of AML in the elderly]. PMID: 36870810
New Checkpoint Inhibitors on the Road: Targeting TIM-3 in Solid Tumors. PMID: 35218498
EXABS-120-MDS Treatment of Higher Risk MDS. PMID: 36163758
EXABS-140-MDS Immune Therapy Approaches in MDS. PMID: 36164227
Management of patients with higher-risk myelodysplastic syndromes after failure of hypomethylating agents: What is on the horizon? PMID: 33762100
Advances in myelodysplastic syndromes: promising novel agents and combination strategies. PMID: 36620919
Current status of phase 3 clinical trials in high-risk myelodysplastic syndromes: pitfalls and recommendations. PMID: 36215988
Biological therapy in elderly patients with acute myeloid leukemia. PMID: 36715330
Modulation of the Gal-9/TIM-3 Immune Checkpoint with α-Lactose. Does Anomery of Lactose Matter? PMID: 34944985

Sabatolimab（MBG453）是直接靶向于TIM-3的人源化的IgG4k抗體，用于治療骨髓增生異常綜合癥（MDS）和急性髓性白血?。ˋML），是一款潛在的“first-in-class”單克隆抗體，可以創(chuàng)新性地同時靶向髓系白血病細(xì)胞和免疫細(xì)胞，不但能殺傷癌細(xì)胞，而且可能增強免疫細(xì)胞的活力。2021年8月，歐盟委員會(EC)已授予諾華sabatolimab治療MDS孤兒藥稱號。2021年12月，在美國血液學(xué)會（ASH）年會公布了sabatolimab聯(lián)合去甲基化藥物（HMAs）治療極高危/高危MDS（vHR/HR-MDS）和AML的療效和安全性試驗數(shù)據(jù)，結(jié)果顯示在接受sabatolimab聯(lián)合HMA治療中：在vHR/HR-MDS患者ORR為56.9%，中位DOR (mDOR) 為16.1個月；CR患者的mDOR為21.5個月（95% CI，12.1-NE）；預(yù)計的12個月PFS 率為51.9%（95% CI，30.6%～69.6%）。在ND-AML患者中，ORR為40.0%，mDOR為12.6個月；CR患者的mDOR為23.0個月（95% CI，1.3～NE）；估計的12個月PFS率為27.9%（95% CI，14.9%~42.5%）。試驗初步證明了sabatolimab + HMA安全且耐受性良好，在vHR/HR-MDS和ND-AML患者中顯示出持久的臨床反應(yīng)，在有不良預(yù)后突變的患者中也顯示出持久的臨床反應(yīng)。