Zoligratinib | Debio 1347 | FGFR Inhibitor | AmBeed-信号通路专用抑制剂

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Zoligratinib 99%+

货号：A120438 同义名： Debio 1347;CH5183284

CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

Zoligratinib 化学结构
CAS号：1265229-25-1

Zoligratinib 3D分子结构
CAS号：1265229-25-1

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Zoligratinib 纯度/质量文件产品仅供科研

货号：A120438 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

FGFR 亚型比较

产品名称	FGFR ↓ ↑	FGFR1 ↓ ↑	FGFR2 ↓ ↑	FGFR3 ↓ ↑	FGFR4 ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ FGFR (Swiss 3T3), IC50: 12.3 μM					PDGFR	99%+
Pazopanib	+ FGFR, IC50: 140 nM						99%
Erdafitinib	✔					RET	99%+
Gambogenic acid	✔						98+%
Sulfatinib		+++ FGFR1, IC50: 15 nM					99+%
Nintedanib esylate		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM			98%
Zoligratinib		+++ FGFR1, IC50: 9.3 nM	+++ FGFR2, IC50: 7.6 nM	++ FGFR3, IC50: 22 nM	+ FGFR4, IC50: 290 nM		99%+
MK-2461		+ FGFR1, IC50: 65 nM	++ FGFR2, IC50: 39 nM	++ FGFR3, IC50: 50 nM			98%+
SU 5402		++ FGFR1, IC50: 30 nM					98%
Brivanib		+ FGFR1, IC50: 148 nM					99%+
Lucitanib		++ FGFR1, IC50: 17.5 nM	+ FGFR2, IC50: 82.5 nM				99%+
Ponatinib		++++ FGFR1, IC50: 2.2 nM					98%
PD-166866		+ FGFR1, IC50: 52.4 nM					98%
Narazaciclib		++ FGFR1, IC50: 26 nM				RET	99%+
Lactate		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	85%
Lenvatinib mesylate		++ FGFR1, IC50: 46 nM				c-RET	99%
LY2874455		++++ FGFR1, IC50: 2.8 nM	++++ FGFR2, IC50: 2.6 nM	+++ FGFR3, IC50: 6.4 nM	+++ FGFR4, IC50: 6 nM		99%+
FIIN-2		+++ FGFR1, IC50: 3.09 nM	+++ FGFR2, IC50: 4.3 nM	++ FGFR3, IC50: 27 nM	++ FGFR4, IC50: 45.3 nM		98%
FIIN-3		+++ FGFR1, IC50: 13.1 nM	++ FGFR2, IC50: 21 nM	++ FGFR3, IC50: 31.4 nM	++ FGFR4, IC50: 35.3 nM		98%
Infigratinib		++++ FGFR1, IC50: 0.9 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM	+ FGFR4, IC50: 60 nM		99%+
Danusertib		++ FGFR1, IC50: 47 nM				RET	99%+
R1530		++ FGFR1, IC50: 28 nM					98%
ENMD-2076		+ FGFR1, IC50: 92.7 nM	+ FGFR2, IC50: 70.8 nM			RET,FLT3	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	99%+
Sorafenib		+ FGFR1, IC50: 580 nM					99%
SSR128129E		+ FGFR1, IC50: 1.9 μM					99%+
AZD-4547		++++ FGFR1, IC50: 0.2 nM	++++ FGFR2, IC50: 2.5 nM	++++ FGFR3, IC50: 1.8 nM			98%
Lenvatinib		++ FGFR1, IC50: 46 nM				RET	98%
PD173074		++ FGFR1, IC50: ~25 nM					99%+
S49076		++ FGFR1, IC50: 18 nM	+++ FGFR2, IC50: 17 nM	+++ FGFR3, IC50: 15 nM			98%
Futibatinib		++++ FGFR1, IC50: 1.8 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.6 nM	+++ FGFR4, IC50: 3.7 nM		99%+
Ferulic Acid		+ FGFR1, IC50: 3.78 μM	+ FGFR2, IC50: 12.5 μM				98%
Nintedanib		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM	+ FGFR4, IC50: 610 nM		99+%
ASP5878		++++ FGFR1, IC50: 0.47 nM	++++ FGFR2, IC50: 0.6 nM	++++ FGFR3, IC50: 0.74 nM	+++ FGFR4, IC50: 3.5 nM		98%
PRN1371		++++ FGFR1, IC50: 0.6 nM	++++ FGFR2, IC50: 1.3 nM	+++ FGFR3, IC50: 4.1 nM	++ FGFR4, IC50: 19.3 nM		99%
Derazantinib		+++ FGFR1, IC50: 4.5 nM	++++ FGFR2, IC50: 1.8 nM	+++ FGFR3, IC50: 4.5 nM	++ FGFR4, IC50: 34 nM	RET	99%+
ODM-203		+++ FGFR1, IC50: 11 nM	+++ FGFR2, IC50: 16 nM	+++ FGFR3, IC50: 6 nM	++ FGFR4, IC50: 35 nM		99%+
Pemigatinib		++++ FGFR1, IC50: 0.4 nM	++++ FGFR2, IC50: 0.5 nM	++++ FGFR3, IC50: 1.2 nM	++ FGFR4, IC50: 30 nM		99%+
SKLB 610			✔			PDGFR	99%+
Alofanib			✔				99%+
Lirafugratinib			✔				98%
Masitinib mesylate				✔		FAK	99%+
BLU9931				+ FGFR3, IC50: 150 nM	+++ FGFR4, IC50: 3 nM		99%+
BO-264				✔			99%+
Fisogatinib					+++ FGFR4, IC50: 5 nM		99%+
H3B-6527					++++ FGFR4, IC50: <1.2 nM		99%+
Roblitinib					++++ FGFR4, IC50: 1.9 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Zoligratinib 生物活性

靶点	FGFR2 FGFR2, IC50:7.6 nM FGFR3 FGFR3, IC50:22 nM FGFR4 FGFR4, IC50:290 nM FGFR1 FGFR1, IC50:9.3 nM
描述	The FGFR (fibroblast growth factor receptor) family, comprising four members, FGFR1, FGFR2, FGFR3 and FGFR4, belongs to the RTKs which serve as high affinity receptors for FGFs controlling cell proliferation, migration, apoptosis and differentiation. CH5183284 is an FGFR-selective inhibitor with IC50 values of 9.3 nM, 7.6 nM, 22 nM and 290 nM for FGFR1, FGFR2, FGFR3 and FGFR4 (measured by enzyme activity), respectively. CH5183284 can prevent auto-phosphorylation of FGFR1, FGFR2, and FGFR3 at 100 to 300 nM in the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification) and KMS11 [t(4;14) translocation and FGFR3 Y373C mutation] cell lines, with no effect on auto-phosphorylation of FGFR4, KDR, PDGFRα, or c-KIT at the same concentration in MDA-MB-453 (FGFR4 mutation), human umbilical vein endothelial cells (HUVEC), NCIH1703 (PDGFRαamplification) and Kasumi-1 (c-KIT N822K mutation). CH5183284 showed more potent inhibition on FGF- than VEGF-dependent proliferation of HUVECs with IC50 of 29 nM, yet had no inhibition on VEGF-induced tube formation of HUVECs. The selective FGFR inhibition by CH5183284 led to the selective antiproliferative activity against the cancer cells harboring the FGFR genetic alterations, including CNV of FGFR1, FGFR1OP-FGFR1, CNVs of FGFR2, FGFR2 (S252W, K310R, N549K), FGFR3-TACC3, FGFR3-BAIAP2L1 and FGFR3 (S249C, Y373C). Oral treatment with CH5183284 at concentration of 10, 30 and 100 mg/kg daily for 11 days caused tumor growth inhibition in a dose-dependent manner in mice bearing KG1, SNU-16, MFE280, UM-UC-14 and RT112/84 harboring the FGFR genetic alterations, but no effect on MKN-45 (cells with MET amplification) xenografted mice. Consistent with in vitro assays, suppression of p-FGFR for at least 7 hours, as well as the downstream signaling, as indicated by a reduction in phospho-FRS, phospho-ERK, and phospho-S6 by CH5183284 can be observed in SNU-16 xenografted tissue^[1].
作用机制	CH5183284 is an ATP-competitive inhibitor through interaction with unique residues in the ATP-binding site of FGFR1, FGFR2, or FGFR3^[1].

Zoligratinib 动物研究

Dose

Mice^[1] (p.o.): 10 mg/kg - 100mg/kg

Administration

p.o.

Pharmacokinetics

Animal	Rats^[1]
Dose	30 mg/kg
Administration	p.o.
AUC	102 mg/h·ml

Zoligratinib 参考文献

[1]Nakanishi Y, Akiyama N, et al. The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther. 2014 Nov;13(11):2547-58.

Zoligratinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.03mL

2.81mL

1.40mL

28.06mL

5.61mL

2.81mL

Zoligratinib 技术信息

CAS号	1265229-25-1
分子式	C₂₀H₁₆N₆O
分子量	356.381

别名	Debio 1347;CH5183284;FF284
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(70.15 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 46 mg/mL suspension

Zoligratinib 99%+

Zoligratinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Zoligratinib 质控信息

Zoligratinib 生物活性

Zoligratinib 动物研究

Zoligratinib 参考文献

Zoligratinib 实验方案

Zoligratinib 技术信息

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FGFR2	FGFR2, IC50:7.6 nM
FGFR3	FGFR3, IC50:22 nM
FGFR4	FGFR4, IC50:290 nM
FGFR1	FGFR1, IC50:9.3 nM

Zoligratinib 99%+

Zoligratinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Zoligratinib 质控信息

Zoligratinib 生物活性

Zoligratinib 动物研究

Zoligratinib 参考文献

Zoligratinib 实验方案

Zoligratinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Zoligratinib 纯度/质量文件产品仅供科研