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Umbralisib
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Umbralisib图片
CAS NO:1532533-67-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Umbralisib (TGR-1202) 是一种具有口服活性、有效和选择性的双重 PI3Kδ 和酪蛋白激酶-1-ε (CK1ε) 抑制剂，EC50 分别为 22.2 nM 和 6.0 μM。 Umbralisib 对慢性淋巴细胞白血病 (CLL) T 细胞具有独特的免疫调节作用。 Umbralisib 可用于血液系统恶性肿瘤研究。
Cas No.1532533-67-7
别名TGR-1202; RP5264
Canonical SMILESO=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3N=C(C4=CC=C(OC(C)C)C(F)=C4)C5=C(N)N=CN=C53)C)OC6=CC=C(F)C=C16
分子式C31H24F3N5O3
分子量571.55
溶解度DMSO : 20 mg/mL (34.99 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TGR-1202 is a PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively.

RP5264 causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[1]. In human lymphoma and leukemia cell lines, TGR-1202 (10 nM-100 uM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. TGR-1202 and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. TGR-1202 and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. TGR-1202 (15-50 uM) 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[2].

In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, TGR-1202 (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2].

References:
[1]. Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth.
[2]. 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