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Itacitinib

Itacitinib (INCB039110) 是一种选择性 JAK1抑制剂，对 人JAK1的IC50值为 2 nM。它对JAK1选择性是 JAK2 的 20 倍多，是 JAK3 和 TYK2 的 100 倍多。

CAS号

1334298-90-6

分子式

C26H23F4N9O

主要靶点

JAK

仅限科研使用

Cat No : CM04895

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Synonyms

INCB039110|伊他替尼|INCB39110

验证数据展示

  • CAS No.: 1334298-90-6

    Itacitinib
    CAS#: 1334298-90-6

产品信息

Itacitinib is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.

CAS号 1334298-90-6
分子式 C26H23F4N9O
主要靶点 JAK
主要通路 干细胞|JAK/STAT信号通路|表观遗传|血管生成
分子量 553.53
纯度 99.01%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 INCB039110|伊他替尼|INCB39110

体内活性

Itacitinib (INCB039110) produced significant improvements in sPGA, demonstrating proof of concept in chronic plaque psoriasis.

体外活性

Itacitinib is an inhibitor of the Janus kinases (JAKs) with selectivity for JAK1.

溶解度

DMSO:30 mg/mL

参考文献

1.Bissonnette R, et al. A randomized, double-blind, placebo-controlled, dose-escalation study of the safety and efficacy of INCB039110, an oral janus kinase 1 inhibitor, in patients with stable, chronic plaque psoriasis. J Dermatolog Treat. 2016 Aug;27(4):332-8.
2.Zhang Y, et al. Impact on creatinine renal clearance by the interplay of multiple renal transporters: a case study with INCB039110. Drug Metab Dispos. 2015 Apr;43(4):485-9.
3.Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia[J]. Cell Death & Disease. 2020, 11(2): 1-11.

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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