LY2874455 | FGFR Inhibitor | AmBeed-信号通路专用抑制剂

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

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		FLT3,c-Kit	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, 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			FLT3,RET	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		FLT3,c-Kit	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。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	c-Kit,FGFR,PDGFR	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms/CSF1R,c-Kit	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 nM	+ hVEGFR3, IC50: 420 nM		99%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2/Flk1, IC50: 90 nM VEGFR2, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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。

靶点	VEGFR2 VEGFR2, IC50:7 nM FGFR2 FGFR2, IC50:2.6 nM FGFR3 FGFR3, IC50:6.4 nM FGFR4 FGFR4, IC50:6 nM FGFR1 FGFR1, IC50:2.8 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. LY2874455 is a pan-FGFR inhibitor with IC50 values of 2.8nM, 2.6nM, 6.4nM and 6nM for FGFR1, 2, 3 and 4, respectively. LY2874455 inhibited p-FGFR2 with estimated IC50 values of 0.8nM and 1.5nM, respectively, in SNU-16 and KATO-III cells, as well as potently inhibit p-ERK induced by FGF2 and FGF9 in a dose-dependent manner, with average IC50 values of 0.3-0.8nM. LY2874455 showed more potent anti-proliferation in cells, such as SNU-16 and KATO-III with a highly amplified fgfr2, suggesting the direct link to the inhibition of FGFR signaling of its antiproliferative effect. LY2874455 exhibited an excellent pharmacokinetic/pharmacodynamic relationship as shown by its dose-dependent inhibition of the tumor growth at TED50 and TED90 (1 and 3 mg/kg, respectively), as well as a rapid, robust, dose-dependent inhibition of tumor growth in SNU-16, OPM-2, NCI-H460 and RT-112 xenograft models especially when dosed at 3 mg/kg twice a day^[1].
作用机制	LY2874455 is an ATP-competitive type of molecule that inhibits FGFR activity via its occupation of the ATP-binding pocket of the enzyme.^[1]

Cell Line RMS559 cells RMS559 cells LPS853 cells LPS510 cells NRH-LS1 cells H1703 H1299 A549 H1299 cells A549 cells H1703 cells KMBC cells KMCH cells NRH-LS1 cells HCC827 cells PC-9 cells Entamoeba invadens trophozoites Entamoeba histolytica trophozoites	Concentration	Treated Time	Description	References
RMS559 cells	100 nM	1 hour	Inhibition of FGFR4 V550L signaling	Br J Cancer. 2022 Nov;127(11):1939-1953.
RMS559 cells	10 nM	72 hours	Inhibition of cell viability	Br J Cancer. 2022 Nov;127(11):1939-1953.
LPS853 cells	100 nM	96 hours	LY2874455 showed modest growth inhibition in LPS853 cells	Cells. 2019 Feb 21;8(2):189.
LPS510 cells	100 nM	96 hours	LY2874455 induced apoptosis in LPS510 cells after 96 hours	Cells. 2019 Feb 21;8(2):189.
NRH-LS1 cells	100 nM	96 hours	LY2874455 induced apoptosis in NRH-LS1 cells after 96 hours	Cells. 2019 Feb 21;8(2):189.
H1703	40 nM	1 hour	To evaluate the effect of LY2874455 on carbon ion radiosensitivity, results showed SER of 1.20±0.18	Int J Mol Sci. 2019 Sep 14;20(18):4563.
H1299	40 nM	1 hour	To evaluate the effect of LY2874455 on carbon ion radiosensitivity, results showed SER of 1.27±0.09	Int J Mol Sci. 2019 Sep 14;20(18):4563.
A549	40 nM	1 hour	To evaluate the effect of LY2874455 on carbon ion radiosensitivity, results showed SER of 1.66±0.17	Int J Mol Sci. 2019 Sep 14;20(18):4563.
H1299 cells	100 nM	1 hour pre-irradiation to 10 days post-irradiation	Evaluate the radiosensitizing effect of LY2874455 on H1299 cells, results showed 100 nM LY2874455 increased the sensitivity of H1299 cells to X-rays by 53%	Cells. 2022 May 24;11(11):1727.
A549 cells	100 nM	1 hour pre-irradiation to 10 days post-irradiation	Evaluate the radiosensitizing effect of LY2874455 on A549 cells, results showed 100 nM LY2874455 increased the sensitivity of A549 cells to X-rays by 62%	Cells. 2022 May 24;11(11):1727.
H1703 cells	100 nM	1 hour pre-irradiation to 10 days post-irradiation	Evaluate the radiosensitizing effect of LY2874455 on H1703 cells, results showed 100 nM LY2874455 increased the sensitivity of H1703 cells to X-rays by 31%	Cells. 2022 May 24;11(11):1727.
KMBC cells	5 µM	24 hours	To evaluate the effect of LY2874455 on cell death in KMBC cells, results showed that LY2874455 induced non-apoptotic cell death.	J Hepatol. 2018 Jun;68(6):1228-1238.
KMCH cells	5 µM	24 hours	To evaluate the effect of LY2874455 on cell death in KMCH cells, results showed that LY2874455 induced non-apoptotic cell death.	J Hepatol. 2018 Jun;68(6):1228-1238.
NRH-LS1 cells	100 nM	72 hours	LY2874455 completely inhibited the growth of NRH-LS1 cells after 72 hours	Cells. 2019 Feb 21;8(2):189.
HCC827 cells	10 nM	72 hours	To evaluate the inhibitory effect of LY2874455 in combination with gefitinib on the proliferation of HCC827 cells. Results showed that LY2874455 significantly reduced the IC50 of gefitinib, effectively reversing gefitinib resistance induced by FGF3/4/19/CCND1 overexpression.	Front Pharmacol. 2022 Jun 23;13:918317.
PC-9 cells	10 nM	72 hours	To evaluate the inhibitory effect of LY2874455 in combination with gefitinib on the proliferation of PC-9 cells. Results showed that LY2874455 significantly reduced the IC50 of gefitinib, effectively reversing gefitinib resistance induced by FGF3/4/19/CCND1 overexpression.	Front Pharmacol. 2022 Jun 23;13:918317.
Entamoeba invadens trophozoites	1.40 µM (EC50)	72 hours	Evaluate the inhibitory effect of LY2874455 on Entamoeba invadens trophozoites, showing micromolar potency.	Antimicrob Agents Chemother. 2022 Feb 15;66(2):e0120721.
Entamoeba histolytica trophozoites	0.31 µM (EC50)	72 hours	Evaluate the inhibitory effect of LY2874455 on Entamoeba histolytica trophozoites, showing submicromolar potency.	Antimicrob Agents Chemother. 2022 Feb 15;66(2):e0120721.

Species NOD/SCID mice BALB/c female nude mice NOD-scid IL2rγnull (NSG) mice BALB/c nude mice Female athymic nude mice	Animal Model Patient-derived xenograft (PDX) model A549 xenograft model LS70x xenograft model PC-9-4X cell xenograft model RMS559 xenograft model	Administration	Dosage	Frequency	Description	References
NOD/SCID mice	Patient-derived xenograft (PDX) model	Oral gavage	3 mg/kg	Twice daily for 7 days	To evaluate the antitumor effect of LY2874455 in the PDX model, results showed that LY2874455 treatment resulted in reduced tumor weight, accompanied by decreased MCL1 expression and cell necrosis.	J Hepatol. 2018 Jun;68(6):1228-1238.
BALB/c female nude mice	A549 xenograft model	Oral	3 mg/kg	Once daily for 7 consecutive days	Evaluate the radiosensitizing effect of LY2874455 on A549 xenograft model, results showed combination treatment significantly suppressed tumor growth without noticeable toxicity	Cells. 2022 May 24;11(11):1727.
NOD-scid IL2rγnull (NSG) mice	LS70x xenograft model	Oral gavage	3 mg/kg	Twice daily for 28 days	LY2874455 significantly inhibited tumor growth in the LS70x xenograft model	Cells. 2019 Feb 21;8(2):189.
BALB/c nude mice	PC-9-4X cell xenograft model	Oral administration	3 mg/kg LY2874455, 100 mg/kg gefitinib, 50 mg/kg abemaciclib	Twice a week for 12 days	To evaluate the inhibitory effect of LY2874455 in combination with gefitinib and abemaciclib on the growth of PC-9-4X xenograft tumors. Results showed that the combination therapy significantly inhibited tumor growth, reduced tumor weight, and decreased Ki67 expression.	Front Pharmacol. 2022 Jun 23;13:918317.
Female athymic nude mice	RMS559 xenograft model	Oral	6 mg/kg	Twice daily (weekdays), once daily (weekends), total of 25 treatments	LY2874455 showed poor efficacy in inhibiting tumor growth in vivo	Br J Cancer. 2022 Nov;127(11):1939-1953.

Dose	Rat^[2] (p.o.): 1 mg/kg - 10 mg/kg
Administration	p.o.

CAS号	1254473-64-7
分子式	C₂₁H₁₉Cl₂N₅O₂
分子量	444.31
SMILES Code	OCCN1N=CC(/C=C/C2=NNC3=C2C=C(O[C@@H](C4=C(Cl)C=NC=C4Cl)C)C=C3)=C1
MDL No.	MFCD22124884

LY2874455 {[allProObj[0].p_purity_real_show]}

LY2874455 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

LY2874455 质控信息

LY2874455 生物活性

LY2874455 细胞实验

LY2874455 动物实验

LY2874455 动物研究

LY2874455 参考文献

LY2874455 实验方案

LY2874455 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

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

别名
运输	蓝冰
InChI Key	GKJCVYLDJWTWQU-CXLRFSCWSA-N
Pubchem ID	46944259

VEGFR2	VEGFR2, IC50:7 nM
FGFR2	FGFR2, IC50:2.6 nM
FGFR3	FGFR3, IC50:6.4 nM
FGFR4	FGFR4, IC50:6 nM
FGFR1	FGFR1, IC50:2.8 nM

LY2874455 {[allProObj[0].p_purity_real_show]}

LY2874455 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

LY2874455 质控信息

LY2874455 生物活性

LY2874455 细胞实验

LY2874455 动物实验

LY2874455 动物研究

LY2874455 参考文献

LY2874455 实验方案

LY2874455 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

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

LY2874455 纯度/质量文件产品仅供科研