Iberdomide|1323403-33-3|-陌孚医药/Medlife

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Iberdomide

目录号: PL01211 纯度: ≥98%

CAS No. :1323403-33-3

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中文名称	Iberdomide
中文别名	(S)-3-(4-((4-(吗啉基甲基)苄基)氧基)-1-氧代异吲哚啉-2-基)哌啶-2,6-二酮
英文名称	Iberdomide
英文别名	Iberdomide;CC 220;CC-220;CC220;8V66F27X44;(S)-3-(4-((4-(Morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione;(3s)-3-[4-({4-[(Morpholin-4-Yl)methyl]phenyl}methoxy)-1-Oxo-1,3-Dihydro-2h-Isoindol-2-Yl]piperidine-2,6-Dione;Iberdomide [USAN];Iberdomide (USAN/INN);GTPL9618;BDBM65497;IXZOHGPZAQLIBH-NRFANRHFSA-N;BCP20299;compound 6 [PMID: 28425720];SB18830;DB12101;D111
Cas No.	1323403-33-3
分子式	C₂₅H₂₇N₃O₅
分子量	449.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Iberdomide (CC-220) 是一种口服有效的 cereblon (CRBN) E3 连接酶调节剂 (CELMoD)，对 cereblon 结合亲和力的 IC₅₀ 为 ~150 nM。Iberdomide 是沙利度胺 (HY-14658) 的衍生物，具有抗肿瘤和免疫刺激活性。

生物活性

Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC 50 of ~150?nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.

性状

Solid

体外研究(In Vitro)

Iberdomide (CC-220; 0.01, 0.1, 1, 10 μM; 72-96 hrs) has antiproliferative effects in a panel of multiple myeloma (MM) cell lines (EJM, H929, KMS11, KMS128M, KMS12PE, MM1.S, MM1.R, RPM-8226, U266 cells) across a range of concentrations.
Iberdomide (0.1 μM; 96 hrs) induces apoptosis in all MM cell lines.
Iberdomide (0.1 μM; 24, 48, 72 hrs) results in time-dependent increases in G0/G1 and sub-G1 cell cycle fractions on H929 cells.
Iberdomide leads to rapid Aiolos depletion in the KMS12BM line.
Iberdomide (0.1 μM) displays some anti-proliferative activity in two of the Pomalidomide-resistant (PR) lines with cereblon mutations (EJM/PR and H929/PR) along with decreased levels of cereblon protein.
Iberdomide (0.1-1000 nM; 72 hrs) equally induces PBMC-mediated killing of both parental MM1.S cells and MM1.S/PR cells.

体内研究(In Vivo)

Iberdomide (CC-220; 10 mg/kg; oral gavage) after 6 or 24 hours causes higher hCRBN expression in hC343 splenocytes correlated to deeper IKZF1/3 downregulation in WT (C57BL/6), hC123, or-343, (representing two different transgenic founder lines expressing hCRBN) and mCrbn mice.
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]. Chad C Bjorklund, et al. Iberdomide (CC-220) is a potent cereblon E3 ligase modulator with antitumor and immunostimulatory activities in lenalidomide- and pomalidomide-resistant multiple myeloma cells with dysregulated CRBN. Leukemia. 2020 Apr;34(4):1197-1201.
[2]. Erin W Meermeier, et al. Tumor burden limits bispecific antibody efficacy through T cell exhaustion averted by concurrent cytotoxic therapy. Blood Cancer Discov. 2021 Jul;2(4):354-369.

溶解度数据	In Vitro: DMSO : 125 mg/mL (278.09 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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