TGR-1202 hydrochloride ( RP5264 hydrochloride | TGR1202 hydrochloride | TGR 1202 hydrochloride )

产品货号. M12156 CAS No. 1532533-78-0

TGR-1202 (RP5264,TGR1202,Umbralisib) 是一种有效的、选择性的、口服的 PI3Kδ 抑制剂，IC50 为 22 nM。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
2MG	￥515	有现货
5MG	￥867	有现货
10MG	￥1720	有现货
100MG	￥7407	有现货
500MG	获取报价	有现货
1G	获取报价	有现货
1 mL x 10 mM in DMSO	￥1378	有现货

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生物学信息

产品名称

TGR-1202 hydrochloride
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

TGR-1202 (RP5264,TGR1202,Umbralisib) 是一种有效的、选择性的、口服的 PI3Kδ 抑制剂，IC50 为 22 nM。
产品描述

TGR-1202 (RP5264,TGR1202,Umbralisib) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM, 50-fold selectivity over PI3Kα/β and >10,000 fold over PI3Kγ; enhances Brentuximab Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest, demonstrates highly synergistic effect with the proteasome inhibitor carfilzomib in lymphoma, leukemia, and myeloma cell lines and primary lymphoma and leukemia cells; synergistically disrupts the 4E-BP1-eIF4F-c-Myc axis with carfilzomib, also potently inhibits 60% of the activity of CK1ε at 1uM.Blood Cancer Phase 3 Clinical
体外实验

Umbralisib hydrochloride causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM.Umbralisib hydrochloride (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner in human lymphoma and leukemia cell lines. Umbralisib hydrochloride (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.
体内实验

Umbralisib hydrochloride (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.
同义词

RP5264 hydrochloride | TGR1202 hydrochloride | TGR 1202 hydrochloride
通路

PI3K/Akt/mTOR signaling
靶点

PI3K
受体

PI3K
研究领域

Cancer
适应症

Blood cancer

化学信息

CAS Number

1532533-78-0
分子量

608.0101
分子式

C31H25ClF3N5O3
纯度

>98% (HPLC)
溶解度

DMSO
SMILES

CC(C)OC1=C(C=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)C4=C(C(=O)C5=C(O4)C=CC(=C5)F)C6=CC(=CC=C6)F)F.Cl
化学全称

4H-1-Benzopyran-4-one, 2-[(1S)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-, hydrochloride (1:1)

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1. Locatelli SL, et al. Leukemia. 2016 Dec;30(12):2402-2405. 2. Deng C, et al. Blood. 2017 Jan 5;129(1):88-99. 3. Burris HA 3rd, et al. Lancet Oncol. 2018 Feb 20. pii: S1470-2045(18)30082-2. 4. Lampson BL, et al. Expert Opin Investig Drugs. 2017 Nov;26(11):1267-1279.

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