Research Grade Sabatolimab
TIM3（CD366；HAVCR2）是一类T细胞表面抑制性分子，能够引起癌症与慢性病毒感染过程中T细胞的衰竭。与CTLA⁃4、PD⁃1类似，TIM3也是目前研究最多的免疫治疗靶点之一。TIM家族由TIM1-TIM8八个成员组成，其中TIM1、TIM3和TIM4在人类中发现。TIM-3由胞外区、跨膜区和胞内区三部分构成，其中胞外区由具有FG-CC’环和N-连接聚糖的N-末端细胞外免疫球蛋白可变区（IgV结构域）、含有O-连接糖基化位点的粘蛋白结构域和含有N-连接聚糖的柄结构域组成，跨膜区由跨膜区组成，胞内区由带有五个酪氨酸残基的胞质尾组成。IgV结构域包含其配体的结合位点。磷脂酰丝氨酸(Ptdser)、癌胚抗原相关细胞粘附分子(CEACAM1)和高迁移率族蛋白1 (HMGB1)结合到FG-CC’环，而Gal9结合到N-连接的聚糖。大量证据表明，TIM基因家族在自身免疫性疾病、感染性疾病、肿瘤免疫监视和免疫逃逸等免疫反应的调节中发挥着不同的作用。TIM3选择性地表达在分泌IFN-γ的T辅助细胞(Th1和Th17) 、T调控细胞(Treg) 、树突状细胞(DCs) 、单核细胞、肥大细胞、NK细胞、肿瘤浸润性淋巴细胞(TILs) 上，在肿瘤细胞上亦有表达，如黑色素瘤、胃癌、B细胞淋巴瘤。
货号：DHJ28402
产品链接：http://www.atagenix.com/product_detail-75240.html
产品购买联系方式：027-65279366
产品介绍：Sabatolimab (MBG453)是一种高亲和力的人源化IgG4 (S228P)抗体，靶向TIM-3，一种调节适应性和先天免疫反应的抑制性受体。Sabatolimab是一种潜在的免疫抑制活性分子，可以靶向免疫细胞和骨髓细胞上的TIM-3。
通用名：Sabatolimab
纯度：>95% by SDS-PAGE.
浓度：1mg/ml
Formulationicon：0.01M PBS, pH 7.4.
内毒素：Please contact with the lab for this information.
别名：MBG-453
靶点;物种：Human CD366/HAVCR2/TIM-3
种类：Humanized
受体鉴定：IgG4-kappa
CAS: 2252262-24-9
存储条件：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.
参考文献：
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抗体，用于治疗骨髓增生异常综合症（MDS）和急性髓性白血病（AML），是一款潜在的“first-in-class”单克隆抗体，可以创新性地同时靶向髓系白血病细胞和免疫细胞，不但能杀伤癌细胞，而且可能增强免疫细胞的活力。2021年8月，欧盟委员会(EC)已授予诺华sabatolimab治疗MDS孤儿药称号。2021年12月，在美国血液学会（ASH）年会公布了sabatolimab联合去甲基化药物（HMAs）治疗极高危/高危MDS（vHR/HR-MDS）和AML的疗效和安全性试验数据，结果显示在接受sabatolimab联合HMA治疗中：在vHR/HR-MDS患者ORR为56.9%，中位DOR (mDOR) 为16.1个月；CR患者的mDOR为21.5个月（95% CI，12.1-NE）；预计的12个月PFS 率为51.9%（95% CI，30.6%～69.6%）。在ND-AML患者中，ORR为40.0%，mDOR为12.6个月；CR患者的mDOR为23.0个月（95% CI，1.3～NE）；估计的12个月PFS率为27.9%（95% CI，14.9%~42.5%）。试验初步证明了sabatolimab + HMA安全且耐受性良好，在vHR/HR-MDS和ND-AML患者中显示出持久的临床反应，在有不良预后突变的患者中也显示出持久的临床反应。
