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CG 428

Cat. No. 7425 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent tropomyosin receptor kinase (TRK) Degrader
化学名： 2-(2,6-Dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-1H-isoindole-1,3(2H)-dione
纯度： ≥98% (HPLC)
说明书
引用文献
评论
文献 (3)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for CG 428

CG 428 is a potent tropomyosin receptor kinase (TRK) Degrader (uSMITE™) (DC50 = 0.36 nM). CG 428 comprises an analog of the pan-TRK inhibitor GNF-8625 joined by a linker to the cereblon E3 ligase ligand pomalidomide (Cat. No. 6302). CG 428 shows selectivity for TRKA over TRKC and TRKB (Kd values = 1nM, 4.2 nM and 28 nM, respectively). Inhibits growth of KM12 colon cancer cells (IC50 =2.9 nM) and is bioavailable.

Negative control CG 428-Neg (Cat. No. 7426), and TrkB antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF1494 and AF397.

许可信息

Sold under license from Cullgen

技术数据 for CG 428

E3 ligase CRBN
DC50 0.36 nM (TMP3-TRKA), 2.23 nM (TRKA) - Degradation in KM12/HEL cells after 6 h treatment
Kd (Degrader to Target) 1 nM - Kd was assessed using the KINOMEscan assay
IC50 (Cellular Activity) 2.9 nM - Inhibits growth of KM12 cells
Selectivity confirmed by global proteomics No
分子量 814.88
公式 C43H43FN10O6
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2412055-93-5
PubChem ID 146410727
InChI Key FWANKJAOTQAHHR-KWRHIPAJSA-N
Smiles FC1=CC=CC([C@H]2CCCN2C3=NN4C(C=C3)=NC=C4C5=NC(N6CCN(C(CCOCCNC7=C8C(N(C(C8=CC=C7)=O)C9CCC(NC9=O)=O)=O)=O)CC6)=CC=C5)=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for CG 428

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 81.49 100

制备储备液 for CG 428

以下数据基于产品分子量 814.88。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.23 mL 6.14 mL 12.27 mL
5 mM 0.25 mL 1.23 mL 2.45 mL
10 mM 0.12 mL 0.61 mL 1.23 mL
50 mM 0.02 mL 0.12 mL 0.25 mL

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参考文献 for CG 428

参考文献是支持产品生物活性的出版物。

Chen et al (2020) Discovery of first-in-class potent and selective tropomyosin receptor kinase degraders. J.Med.Chem. 63 14562 PMID: 33058680

If you know of a relevant reference for CG 428, please let us know.

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关键词: CG 428, CG 428 supplier, CG428, degraders, uSMITE, E3, ligase, TRK, tropomyosin, receptors, kinases, potent, selective, PROTAC, targeted, protein, degradation, Ubiquitin-mediated, Small, Molecule-Induced, Target, Elimination, Other, Kinases, Raf, and, Ras, Degraders, 7425, Tocris Bioscience

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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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