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Taminadenant Sale

(Synonyms: 5-溴-2,6-二(1-H吡唑)基-4-氨基嘧啶,NIR178; PBF509) 目录号 : GC64943

Taminadenant 是腺苷受体 (adenosine receptor) 的拮抗剂。

Taminadenant Chemical Structure

Cas No.:1337962-47-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,089.00
现货
5mg
¥990.00
现货
10mg
¥1,440.00
现货
50mg
¥4,410.00
现货
100mg
¥7,110.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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产品描述

Taminadenant is an antagonist of adenosine receptor[1].

[1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, 2018, 32(4).

Chemical Properties

Cas No. 1337962-47-6 SDF Download SDF
别名 5-溴-2,6-二(1-H吡唑)基-4-氨基嘧啶,NIR178; PBF509
分子式 C10H8BrN7 分子量 306.12
溶解度 DMSO : 125 mg/mL (408.34 mM; Need ultrasonic) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.2667 mL 16.3335 mL 32.6669 mL
5 mM 0.6533 mL 3.2667 mL 6.5334 mL
10 mM 0.3267 mL 1.6333 mL 3.2667 mL
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Research Update

Phase I Study of Taminadenant (PBF509/NIR178), an Adenosine 2A Receptor Antagonist, with or without Spartalizumab (PDR001), in Patients with Advanced Non-Small Cell Lung Cancer

Clin Cancer Res 2022 Jun 1;28(11):2313-2320.PMID:35254415DOI:PMC9167697

Purpose: The adenosine 2A receptor (A2AR) mediates the immunosuppressive effects of adenosine in the tumor microenvironment and is highly expressed in non-small cell lung cancer (NSCLC). Taminadenant (PBF509/NIR178) is an A2AR antagonist able to reactivate the antitumor immune response. Patients and methods: In this phase I/Ib, dose-escalation/expansion study, patients with advanced/metastatic NSCLC and ≥1 prior therapy received Taminadenant (80-640 mg, orally, twice a day) with or without spartalizumab (anti-programmed cell death-1, 400 mg, i.v., every 4 weeks). Primary endpoints were safety, tolerability, and feasibility of the combination. Results: During dose escalation, 25 patients each received Taminadenant alone or with spartalizumab; 19 (76.0%) and 9 (36.0%) had received prior immunotherapy, respectively. Dose-limiting toxicities (all Grade 3) with Taminadenant alone were alanine/aspartate aminotransferase increase and nausea [n = 1 (4.0%) each; 640 mg], and in the combination group were pneumonitis [n = 2 (8.0%); 160 and 240 mg] and fatigue and alanine/aspartate aminotransferase increase [n = 1 (4.0%) each; 320 mg]; pneumonitis cases responded to steroids rapidly and successfully. Complete and partial responses were observed in one patient each in the single-agent and combination groups; both were immunotherapy naïve. In the single-agent and combination groups, 7 and 14 patients experienced stable disease; 7 and 6 patients were immunotherapy pretreated, respectively. Conclusions: Taminadenant, with and without spartalizumab, was well tolerated in patients with advanced NSCLC. The maximum tolerated dose of Taminadenant alone was 480 mg twice a day, and 240 mg twice a day plus spartalizumab. Efficacy was neither a primary or secondary endpoint; however, some clinical benefit was noted regardless of prior immunotherapy or programmed cell death ligand-1 status.