1. Immunology/Inflammation Protein Tyrosine Kinase/RTK
  2. IRAK FLT3
  3. Emavusertib hydrochloride

Emavusertib hydrochloride  (Synonyms: CA-4948 hydrochloride)

目录号: HY-135317B
产品使用指南

Emavusertib (CA-4948) hydrochloride 是一种选择性、有效且具有口服活性的 IRAK4/FLT3 抑制剂。 在 FRET 激酶测定中,Emavusertib hydrochloride 对 IRAK4IC50 为 57 nM。 Emavusertib hydrochloride 显示出抗肿瘤活性。

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Emavusertib hydrochloride Chemical Structure

Emavusertib hydrochloride Chemical Structure

CAS No. : 2376399-42-5

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Emavusertib hydrochloride 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3].

IC50 & Target

IRAK4

57 nM (IC50)

体外研究
(In Vitro)

Emavusertib 对 IRAK-4 的结合亲和力比对 IRAK 1、2 和 3 的结合亲和力高出 350 倍以上[3]
Emavusertib (10 μM, 72 h) 可降低边缘区淋巴瘤 (MZL) 细胞系中增殖细胞的百分比并诱导亚 G0 分数适度增加[3]
Emavusertib (10 μM, 72 h) 可诱导 MZL 细胞凋亡细胞群显著增加,尤其是与 Ibrutinib (HY-10997) 联合使用时[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Emavusertib (25-150 mg/kg,口服,每日一次,连续 14 天)可诱导小鼠肿瘤生长抑制[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice bearing OCI-LY10 tumors[3]
Dosage: 25, 50, or 150 mg/kg (once daily), 12.5, 25, or 50 mg/kg (twice daily)
Administration: Orally, once daily or twice daily, for 14 consecutive days
Result: Induced tumor growth inhibition. Emavusertib administered as a twice-daily divided dose was equivalent to the corresponding once-daily dose with regards to antitumor activity, i.e., 12.5 mg/kg BID versus 25 mg/kg QD.
分子量

527.96

Formula

C24H26ClN7O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

Emavusertib hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Emavusertib hydrochloride
目录号:
HY-135317B
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