Umbralisib|1532533-67-7|(TGR-1202; RP5264)-陌孚医药/Medlife

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Umbralisib (Synonyms: TGR-1202; RP5264)

目录号: PL09817 纯度: ≥98%

CAS No. :1532533-67-7

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中文名称	Umbralisib
中文别名	TGR-1202
英文名称	Umbralisib
英文别名	TGR-1202;RP5264;RP-5264;TGR1202;Umbralisib;(S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one;38073MQB2A;AK173784;Umbralisib [USAN];Umbralisib (USAN/INN);GTPL8916;TGR 1202 [WHO-DD];IUVCFHHAEHNCFT-INIZCTEOSA-N;BDBM184556;2-[(1S)-1-[4-amino-3-(3-fluoro-4-propan-2-yloxyphenyl)pyrazolo[3,4-d]pyrimidi
Cas No.	1532533-67-7
分子式	C₃₁H₂₄F₃N₅O₃
分子量	571.55
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Umbralisib (TGR-1202) 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 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 可用于血液系统恶性肿瘤的研究。

生物活性

Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC 50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach.

性状

Solid

IC50 & Target[1][2]

PI3Kδ 22.2 nM (EC50) PI3Kδ 6.2 nM (Kd)p

体外研究(In Vitro)

Umbralisib causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM.
Umbralisib (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner in human lymphoma and leukemia cell lines.
Umbralisib (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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 25 mg/mL (43.74 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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