Umbralisib sulfate(Synonyms: TGR-1202 sulfate)

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Umbralisib sulfate (Synonyms: TGR-1202 sulfate)

Umbralisib sulfate 是一种具有口服有效、选择性的双 PI3Kδ 和 酪蛋白激酶-1-ε (CK1ε) 抑制剂，其 EC50 分别为 22.2 nM 和 6.0 μM。 Umbralisib sulfate 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 sulfate 可用于血液系统恶性肿瘤的研究。

Umbralisib sulfate(Synonyms: TGR-1202 sulfate)

Umbralisib sulfate Chemical Structure

CAS No. : 1532533-75-7

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Umbralisib sulfate 的其他形式现货产品:

Umbralisib Umbralisib hydrochloride

生物活性

Umbralisib sulfate 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 sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach[1][2][3][4].

IC50 & Target

PI3Kδ

6.2 (Kd)

CK1ϵ

180 (Kd)

PI3Kγ

1400 (Kd)

PI3Kα

>10000 (Kd)

PI3Kβ

>10000 (Kd)

体外研究
(In Vitro)

Umbralisib sulfatecauses a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[3].
In human lymphoma and leukemia cell lines, Umbralisib sulfate (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner[4].
Umbralisib sulfate (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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

669.63

Formula

C31H26F3N5O7S
CAS 号

1532533-75-7
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.
参考文献

  • [1]. Maharaj K, et al. The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells. Blood Adv. 2020 Jul 14;4(13):3072-3084.

    [2]. Burris HA 3rd, et al. Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study. Lancet Oncol. 2018 Apr;19(4):486-496.

    [3]. Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth.

    [4]. Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99.

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