1. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage
  2. PI3K Casein Kinase
  3. Umbralisib tosylate

Umbralisib tosylate  (Synonyms: TGR-1202 tosylate; RP5264 tosylate)

目录号: HY-12279A
产品使用指南

Umbralisib (TGR-1202) tosylate 是一种口服有效、选择性的 PI3Kδ 和 酪蛋白激酶-1-ε (CK1ε) 双抑制剂,其 EC50 分别为 22.2 nM 和 6.0 μM。 Umbralisib tosylate 显示出对慢性淋巴细胞白血病 (CLL) T 细胞独特的免疫调节作用。Umbralisib tosylate 可用于血液系统恶性肿瘤的研究。

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Umbralisib tosylate Chemical Structure

Umbralisib tosylate Chemical Structure

CAS No. : 1532533-72-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach[1][2][3][4].

IC50 & Target

PI3Kδ

6.2 nM (Kd)

PI3Kγ

1400 nM (Kd)

PI3Kβ

>10000 nM (Kd)

PI3Kα

>10000 nM (Kd)

体外研究
(In Vitro)

Umbralisib tosylate causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[3].
Umbralisib tosylate (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner in human lymphoma and leukemia cell lines[4].
Umbralisib tosylate (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells[4].

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

体内研究
(In Vivo)

Umbralisib tosylate (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25 in a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line[4].

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

Clinical Trial
分子量

743.75

Formula

C38H32F3N5O6S

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
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  • 稀释计算器

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

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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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Umbralisib tosylate
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HY-12279A
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