Pemigatinib | INCB054828 | FGFR Inhibitor | AmBeed-信号通路专用抑制剂

Pemigatinib/培米加替尼 {[allProObj[0].p_purity_real_show]}

货号：A1176662 同义名： INCB054828

Pemigatinib是口服生物可利用的纤维母细胞生长因子受体（FGFR）类型 1、2、3（FGFR1/2/3）抑制剂，具有潜在的抗肿瘤活性。Pemigatinib 通过与 FGFR1/2/3 结合并抑制其功能，可能会抑制 FGFR1/2/3 相关的信号转导通路，从而抑制在 FGFR1/2/3 过度表达的肿瘤细胞中的增殖。

Pemigatinib/培米加替尼化学结构
CAS号：1513857-77-6

Pemigatinib/培米加替尼 3D分子结构
CAS号：1513857-77-6

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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					99%
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		99%
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 (K650E), IC50: 4.9 nM FGFR3, IC50: 1.0 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		99%
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			✔				99%
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。

Pemigatinib/培米加替尼生物活性

靶点

FGFR2

FGFR2, IC50:0.5 nM
FGFR3

FGFR3, IC50:1.2 nM
FGFR4

FGFR4, IC50:30 nM
FGFR1

FGFR1, IC50:0.4 nM

描述

Fibroblast growth factor receptor (FGFR) tyrosine kinases, which are expressed on the cell membrane, are involved in a wide range of biological functions such as cell proliferation, survival, migration, and differentiation. The identification of FGFR fusions and other alterations in a wide range of solid tumors, including cholangiocarcinoma and bladder cancer, has resulted in the development of several selective FGFR inhibitors for use in these indications, for example, infigratinib, erdafitinib, derazantinib, pemigatinib, and futibatinib^[1]. Pemigatinib is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) types 1, 2, and 3, with potential antineoplastic activity^[2]. It is used for the treatment of adults with previously treated, unresectable, locally advanced or metastatic cholangiocarcinoma and a FGFR2 fusion or other rearrangement (13.5mg once daily)^[3]. Pemigatinib was investigated using xenograft tumor models with genetic alterations in FGFR1, 2, or 3. Enzymatic assays with recombinant human FGFR kinases showed potent inhibition of FGFR1, 2, and 3 by Pemigatinib (half maximal inhibitory concentration [IC50] 0.4, 0.5, and 1.0 nM, respectively) with weaker activity against FGFR4 (IC50 30 nM). Pemigatinib selectively inhibited growth of tumor cell lines with activation of FGFR signaling. The preclinical pharmacokinetic profile suggests target inhibition is achievable by Pemigatinib in vivo with low oral doses and the combination of Pemigatinib with cisplatin provided significant benefit over either single agent, with an acceptable tolerability^[4].

Pemigatinib/培米加替尼细胞实验

Cell Line PDC-DUC18828 PDO-DUC18828 primary mouse astrocytes primary human astrocytes ICC13-7 cells ICC21 cells NCI-H1581 lung cancer cells KATO III gastric cancer cells RT-112 bladder cancer cells EC PDXOs ICC13-7 ICC21 NCI-H1581 lung cancer cells KATO III gastric cancer cells RT-112 bladder cancer cells	Concentration	Treated Time	Description	References
PDC-DUC18828	4 nM	3 days	To evaluate the inhibitory effect of Pemigatinib on the growth and proliferation of FGFR2 fusion-positive ICC cell lines, results showed that Pemigatinib significantly inhibited cell proliferation at low nanomolar concentrations	NPJ Precis Oncol. 2022 Oct 23;6(1):75.
PDO-DUC18828	2 nM	7 days	To evaluate the inhibitory effect of Pemigatinib on the growth and proliferation of FGFR2 fusion-positive ICC organoids, results showed that Pemigatinib significantly inhibited organoid growth at low nanomolar concentrations	NPJ Precis Oncol. 2022 Oct 23;6(1):75.
primary mouse astrocytes	100 nM, 1 μM, 10 μM	24 h	Pemigatinib attenuated proinflammatory signaling (Csf2, Tnf, Ccl2, Ccl5, Cxcl10).	JCI Insight. 2022 Apr 8;7(7):e154824.
primary human astrocytes	10 μM	24 h	Pemigatinib treatment attenuated proinflammatory signaling but did not significantly affect cell survival.	JCI Insight. 2022 Apr 8;7(7):e154824.
ICC13-7 cells	100 nM	24 h	To investigate the effect of Pemigatinib on glycolytic gene expression, results showed that Pemigatinib significantly suppressed glycolytic gene expression.	Nat Commun. 2024 May 7;15(1):3805.
ICC21 cells	100 nM	24 h	To investigate the effect of Pemigatinib on glycolytic gene expression, results showed that Pemigatinib significantly suppressed glycolytic gene expression.	Nat Commun. 2024 May 7;15(1):3805.
NCI-H1581 lung cancer cells	100 nM	24 and 48 h	Pemigatinib significantly reduced the proliferative ability of NCI-H1581 lung cancer cells, induced G1 phase cell cycle arrest, and triggered apoptosis.	J Transl Med. 2023 Sep 15;21(1):626.
KATO III gastric cancer cells	100 nM	24 and 48 h	Pemigatinib significantly reduced the proliferative ability of KATO III gastric cancer cells, induced G1 phase cell cycle arrest, and triggered senescence.	J Transl Med. 2023 Sep 15;21(1):626.
RT-112 bladder cancer cells	100 nM	24 and 48 h	Pemigatinib significantly reduced the proliferative ability of RT-112 bladder cancer cells, induced G1 phase cell cycle arrest, and triggered apoptosis.	J Transl Med. 2023 Sep 15;21(1):626.
EC PDXOs	300 nM	72 h	To evaluate the effect of Pemigatinib on cell death in EC PDXOs, significant cell death was observed in models with high FGFR2c expression.	NPJ Precis Oncol. 2023 Dec 8;7(1):127.
ICC13-7	100 nM	5 days	To evaluate the sensitivity of FGFR2 fusion-positive ICC cell lines to Pemigatinib, results showed that ICC13-7 cells were highly sensitive to Pemigatinib with an IC50 of 12 nM.	Cancer Discov. 2022 May 2;12(5):1378-1395.
ICC21	100 nM	5 days	To evaluate the sensitivity of FGFR2 fusion-positive ICC cell lines to Pemigatinib, results showed that ICC21 cells were partially sensitive to Pemigatinib with an IC50 of ~250 nM.	Cancer Discov. 2022 May 2;12(5):1378-1395.
NCI-H1581 lung cancer cells	100 nM	24 and 48 h	Pemigatinib significantly reduced the proliferative ability of NCI-H1581 lung cancer cells, inducing G1 phase cell cycle arrest and apoptosis.	J Transl Med. 2023 Sep 15;21(1):626.
KATO III gastric cancer cells	100 nM	24 and 48 h	Pemigatinib significantly reduced the proliferative ability of KATO III gastric cancer cells, inducing G1 phase cell cycle arrest and senescence.	J Transl Med. 2023 Sep 15;21(1):626.
RT-112 bladder cancer cells	100 nM	24 and 48 h	Pemigatinib significantly reduced the proliferative ability of RT-112 bladder cancer cells, inducing G1 phase cell cycle arrest and increasing intracellular ROS production.	J Transl Med. 2023 Sep 15;21(1):626.

Cell Line

Concentration

Treated Time

Description

References

PDC-DUC18828

4 nM

3 days

To evaluate the inhibitory effect of Pemigatinib on the growth and proliferation of FGFR2 fusion-positive ICC cell lines, results showed that Pemigatinib significantly inhibited cell proliferation at low nanomolar concentrations

NPJ Precis Oncol. 2022 Oct 23;6(1):75.

PDO-DUC18828

2 nM

7 days

To evaluate the inhibitory effect of Pemigatinib on the growth and proliferation of FGFR2 fusion-positive ICC organoids, results showed that Pemigatinib significantly inhibited organoid growth at low nanomolar concentrations

NPJ Precis Oncol. 2022 Oct 23;6(1):75.

primary mouse astrocytes

100 nM, 1 μM, 10 μM

24 h

Pemigatinib attenuated proinflammatory signaling (Csf2, Tnf, Ccl2, Ccl5, Cxcl10).

JCI Insight. 2022 Apr 8;7(7):e154824.

primary human astrocytes

10 μM

24 h

Pemigatinib treatment attenuated proinflammatory signaling but did not significantly affect cell survival.

JCI Insight. 2022 Apr 8;7(7):e154824.

ICC13-7 cells

100 nM

24 h

To investigate the effect of Pemigatinib on glycolytic gene expression, results showed that Pemigatinib significantly suppressed glycolytic gene expression.

Nat Commun. 2024 May 7;15(1):3805.

ICC21 cells

100 nM

24 h

To investigate the effect of Pemigatinib on glycolytic gene expression, results showed that Pemigatinib significantly suppressed glycolytic gene expression.

Nat Commun. 2024 May 7;15(1):3805.

NCI-H1581 lung cancer cells

100 nM

24 and 48 h

Pemigatinib significantly reduced the proliferative ability of NCI-H1581 lung cancer cells, induced G1 phase cell cycle arrest, and triggered apoptosis.

J Transl Med. 2023 Sep 15;21(1):626.

KATO III gastric cancer cells

100 nM

24 and 48 h

Pemigatinib significantly reduced the proliferative ability of KATO III gastric cancer cells, induced G1 phase cell cycle arrest, and triggered senescence.

J Transl Med. 2023 Sep 15;21(1):626.

RT-112 bladder cancer cells

100 nM

24 and 48 h

Pemigatinib significantly reduced the proliferative ability of RT-112 bladder cancer cells, induced G1 phase cell cycle arrest, and triggered apoptosis.

J Transl Med. 2023 Sep 15;21(1):626.

EC PDXOs

300 nM

72 h

To evaluate the effect of Pemigatinib on cell death in EC PDXOs, significant cell death was observed in models with high FGFR2c expression.

NPJ Precis Oncol. 2023 Dec 8;7(1):127.

ICC13-7

100 nM

5 days

To evaluate the sensitivity of FGFR2 fusion-positive ICC cell lines to Pemigatinib, results showed that ICC13-7 cells were highly sensitive to Pemigatinib with an IC50 of 12 nM.

Cancer Discov. 2022 May 2;12(5):1378-1395.

ICC21

100 nM

5 days

To evaluate the sensitivity of FGFR2 fusion-positive ICC cell lines to Pemigatinib, results showed that ICC21 cells were partially sensitive to Pemigatinib with an IC50 of ~250 nM.

Cancer Discov. 2022 May 2;12(5):1378-1395.

NCI-H1581 lung cancer cells

100 nM

24 and 48 h

Pemigatinib significantly reduced the proliferative ability of NCI-H1581 lung cancer cells, inducing G1 phase cell cycle arrest and apoptosis.

J Transl Med. 2023 Sep 15;21(1):626.

KATO III gastric cancer cells

100 nM

24 and 48 h

Pemigatinib significantly reduced the proliferative ability of KATO III gastric cancer cells, inducing G1 phase cell cycle arrest and senescence.

J Transl Med. 2023 Sep 15;21(1):626.

RT-112 bladder cancer cells

100 nM

24 and 48 h

Pemigatinib significantly reduced the proliferative ability of RT-112 bladder cancer cells, inducing G1 phase cell cycle arrest and increasing intracellular ROS production.

J Transl Med. 2023 Sep 15;21(1):626.

Pemigatinib/培米加替尼动物实验

Species Mice Mice Mice Mice Mice Mice	Animal Model Subcutaneous xenograft model Liver fibrosis model Experimental autoimmune encephalomyelitis (EAE) model PDX models EC PDX models ICC11 subcutaneous xenograft model	Administration	Dosage	Frequency	Description	References
Mice	Subcutaneous xenograft model	Oral	5 mg/kg	5 days per week, continuous treatment	To evaluate the inhibitory effect of Pemigatinib on the growth of FGFR2 fusion-positive ICC xenografts, results showed that Pemigatinib significantly inhibited tumor growth and prolonged the survival of mice	NPJ Precis Oncol. 2022 Oct 23;6(1):75.
Mice	Liver fibrosis model	Intraperitoneal injection	0.3 mg/kg	Once daily for 8 weeks	To study the effect of Pemigatinib on liver fibrosis model mice, it was found that Pemigatinib significantly alleviated liver fibrosis and improved bone density and microstructure damage.	Hepatol Commun. 2025 Jan 7;9(1):e0610.
Mice	Experimental autoimmune encephalomyelitis (EAE) model	Intranasal administration	2.5 mg/kg	Daily until the end of the experiment	Pemigatinib had no significant effect on the EAE disease course.	JCI Insight. 2022 Apr 8;7(7):e154824.
Mice	PDX models	Oral	1 mg/kg	Daily for 11 days	To investigate the effect of Pemigatinib on glycolytic gene expression, results showed that Pemigatinib significantly suppressed glycolytic gene expression.	Nat Commun. 2024 May 7;15(1):3805.
Mice	EC PDX models	Oral	1 mg/kg	Once daily for 21 days	To evaluate the tumor growth inhibition effect of Pemigatinib in EC PDX models, significant tumor growth inhibition and prolonged survival were observed in 4/5 models.	NPJ Precis Oncol. 2023 Dec 8;7(1):127.
Mice	ICC11 subcutaneous xenograft model	Oral	1 mg/kg	Once daily for 10 days with 4-day intervals	To evaluate the in vivo efficacy of Pemigatinib in combination with Afatinib in FGFR2 fusion-positive ICC models, results showed that the combination treatment significantly inhibited tumor growth.	Cancer Discov. 2022 May 2;12(5):1378-1395.

Species

Mice Mice Mice Mice Mice Mice

Animal Model

Subcutaneous xenograft model Liver fibrosis model Experimental autoimmune encephalomyelitis (EAE) model PDX models EC PDX models ICC11 subcutaneous xenograft model

Administration

Dosage

Frequency

Description

References

Mice

Subcutaneous xenograft model

Oral

5 mg/kg

5 days per week, continuous treatment

To evaluate the inhibitory effect of Pemigatinib on the growth of FGFR2 fusion-positive ICC xenografts, results showed that Pemigatinib significantly inhibited tumor growth and prolonged the survival of mice

NPJ Precis Oncol. 2022 Oct 23;6(1):75.

Mice

Liver fibrosis model

Intraperitoneal injection

0.3 mg/kg

Once daily for 8 weeks

To study the effect of Pemigatinib on liver fibrosis model mice, it was found that Pemigatinib significantly alleviated liver fibrosis and improved bone density and microstructure damage.

Hepatol Commun. 2025 Jan 7;9(1):e0610.

Mice

Experimental autoimmune encephalomyelitis (EAE) model

Intranasal administration

2.5 mg/kg

Daily until the end of the experiment

Pemigatinib had no significant effect on the EAE disease course.

JCI Insight. 2022 Apr 8;7(7):e154824.

Mice

PDX models

Oral

1 mg/kg

Daily for 11 days

To investigate the effect of Pemigatinib on glycolytic gene expression, results showed that Pemigatinib significantly suppressed glycolytic gene expression.

Nat Commun. 2024 May 7;15(1):3805.

Mice

EC PDX models

Oral

1 mg/kg

Once daily for 21 days

To evaluate the tumor growth inhibition effect of Pemigatinib in EC PDX models, significant tumor growth inhibition and prolonged survival were observed in 4/5 models.

NPJ Precis Oncol. 2023 Dec 8;7(1):127.

Mice

ICC11 subcutaneous xenograft model

Oral

1 mg/kg

Once daily for 10 days with 4-day intervals

To evaluate the in vivo efficacy of Pemigatinib in combination with Afatinib in FGFR2 fusion-positive ICC models, results showed that the combination treatment significantly inhibited tumor growth.

Cancer Discov. 2022 May 2;12(5):1378-1395.

Pemigatinib/培米加替尼参考文献

Pemigatinib/培米加替尼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.26mL

2.05mL

1.03mL

20.51mL

4.10mL

2.05mL

Pemigatinib/培米加替尼技术信息

CAS号	1513857-77-6
分子式	C₂₄H₂₇F₂N₅O₄
分子量	487.5
SMILES Code	FC1=C(C(F)=C(OC)C=C1OC)N(CC2=CNC3=NC(CN4CCOCC4)=CC3=C25)C(N5CC)=O
MDL No.	MFCD31706227

别名	INCB054828
运输	蓝冰
InChI Key	HCDMJFOHIXMBOV-UHFFFAOYSA-N
Pubchem ID	86705695

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 25 mg/mL(51.28 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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

方案四

靶点

靶点	数值

FGFR2	FGFR2, IC50:0.5 nM
FGFR3	FGFR3, IC50:1.2 nM
FGFR4	FGFR4, IC50:30 nM
FGFR1	FGFR1, IC50:0.4 nM

Pemigatinib/培米加替尼 {[allProObj[0].p_purity_real_show]}

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Pemigatinib/培米加替尼细胞实验

Pemigatinib/培米加替尼动物实验

Pemigatinib/培米加替尼参考文献

Pemigatinib/培米加替尼实验方案

Pemigatinib/培米加替尼技术信息

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全球学术期刊中引用的产品

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Pemigatinib/培米加替尼 细胞实验

Pemigatinib/培米加替尼 动物实验

Pemigatinib/培米加替尼 参考文献

Pemigatinib/培米加替尼 实验方案

Pemigatinib/培米加替尼 技术信息

最近浏览的产品

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摩尔计算器

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临床研究

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Pemigatinib/培米加替尼动物实验

Pemigatinib/培米加替尼参考文献

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