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Umbralisib Sale

(Synonyms: TGR-1202; RP5264) 目录号 : GC19355

A PI3K p110δ inhibitor

Umbralisib Chemical Structure

Cas No.:1532533-67-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥968.00
现货
1mg
¥350.00
现货
5mg
¥770.00
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10mg
¥1,330.00
现货
25mg
¥3,080.00
现货
50mg
¥4,060.00
现货
100mg
¥6,930.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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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

Chemical Properties

Cas No. 1532533-67-7 SDF
别名 TGR-1202; RP5264
Canonical SMILES O=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
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.7496 mL 8.7481 mL 17.4963 mL
5 mM 0.3499 mL 1.7496 mL 3.4993 mL
10 mM 0.175 mL 0.8748 mL 1.7496 mL
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