Safimaltib|2230273-76-2|(JNJ-67856633)-陌孚医药/Medlife

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Safimaltib (Synonyms: JNJ-67856633)

目录号: PL06920 纯度: ≥99%

CAS No. :2230273-76-2

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中文名称	Safimaltib
英文名称	Safimaltib
英文别名	L9790S42AI;1-(1-Oxo-1,2-dihydroisoquinolin-5-yl)-5-(trifluoromethyl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1H-pyrazole-4-carboxamide;1-(1-oxo-2H-isoquinolin-5-yl)-5-(trifluoromethyl)-N-[2-(trifluoromethyl)pyridin-4-yl]pyrazole-4-carb;Safimaltib
Cas No.	2230273-76-2
分子式	C₂₀H₁₁F₆N₅O₂
分子量	467.32
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Safimaltib (JNJ-67856633) 是一种具有口服活性、第一类、有效、选择性和变构性 MALT1 protease 抑制剂。Safimaltib 在某些情况下导致肿瘤停滞。

生物活性

Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis.

性状

Solid

IC50 & Target[1][2]

MALT1 protease

体外研究(In Vitro)

Safimaltib (JNJ-67856633) is effective and highly bioavailable in both mouse and rat tumors, and in some cases led to tumor stasis.
Safimaltib leads to potent in vivo pharmacodynamic shutdown in CD79b- as well as CARD11-mutant ABC-DLBCL models as measured by serum IL10 or uncleaved BCL10 levels in tumors. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Dose dependent inhibition of the generation of Tregs (CD4CD25FoxP3) following CD3/28 stimulation was observed upon treatment with JNJ-67856633 suggesting a potential immune modulatory role of MALT1 inhibition. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Virtual meeting delivers first time drug structures
[2]. A Phase 1, First-in-Human, Open-Label Study of the Safety, Pharmacokinetics, and Pharmacodynamics of JNJ-67856633, an Inhibitor of MALT1, in Participants with NHL and CLL
[3]. Abstract 5690: Discovery of JNJ-67856633: A novel, first-in-class MALT1 protease inhibitor for the treatment of B cell lymphomas

溶解度数据	In Vitro: DMSO : 125 mg/mL (267.48 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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