货号:A410196
同义名:
E-3810; Lucitanib hydrochloride
Lucitanib是一种 VEGFR 和 FGFR 的双重抑制剂,能强效选择性抑制 VEGFR1、VEGFR2、VEGFR3、FGFR1 和 FGFR2,IC50 分别为 7 nM、25 nM、10 nM、17.5 nM 和 82.5 nM。


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| 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 |
RET,FLT3 | 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, IC50: 3 nM VEGFR2/Flk1, 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 |
FGFR,PDGFR,c-Kit | 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, IC50: 90 nM VEGFR2/Flk1, 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 |
RET,FLT3 | 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 |
|
| 描述 | E-3810 is a dual inhibitor of the VEGF and FGF receptors, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. |
| Concentration | Treated Time | Description | References | |
| Baf3-CCDC6-RET cells | 1–10 μmol/L | AL3810 dose-dependently inhibited the proliferation of Baf3-CCDC6-RET cells with an IC50 value of 2.77 μmol/L. | Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542 | |
| TPC-1 cells | 2–5 μmol/L | 72 hours | AL3810 dose-dependently inhibited the proliferation of TPC-1 cells with IC50 values ranging from 0.59 to 7.03 μmol/L. | Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542 |
| SW579 cells | 2–5 μmol/L | 72 hours | AL3810 dose-dependently inhibited the proliferation of SW579 cells with IC50 values ranging from 0.59 to 7.03 μmol/L. | Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542 |
| TT cells | 2–5 μmol/L | 72 hours | AL3810 dose-dependently inhibited the proliferation of TT cells with IC50 values ranging from 0.59 to 7.03 μmol/L. | Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542 |
| Small cell lung cancer cell line (DMS114) | 1μM | 4, 24, 48 and 72 hours | To study the effect of Lucitanib on cell cycle in FGFR1 amplified cell lines. Results showed a G1 block in DMS114 cells from 24 to 48 hours, but no apoptosis was detected. | Neoplasia. 2017 Jan;19(1):35-42 |
| Non-small cell lung cancer cell lines (H1299, H1975, H2342, H1650, H358, A549, H2228, H23, H1581, H520) | 0.01 to 50μM | 72 hours | To evaluate the growth inhibitory effect of Lucitanib on cell lines with FGFR1/2 amplification or mutation. Results showed that FGFR1/2 amplified or mutated cell lines were more sensitive to Lucitanib (IC50 of 0.045–3.16μM) compared to wild-type cell lines (IC50 of 3–23μM). | Neoplasia. 2017 Jan;19(1):35-42 |
| CAMA1 cells | 1 μM | 6 days | Lucitanib combined with fulvestrant/palbociclib significantly inhibited cell growth, inducing cell cycle arrest and senescence | Nat Commun. 2019 Mar 26;10(1):1373 |
| T47D cells | 1 μM | 14 days | FGFR1 overexpression confers resistance to fulvestrant ± palbociclib, which was reversed by lucitanib | Nat Commun. 2019 Mar 26;10(1):1373 |
| MCF-7 cells | 1 μM | 14 days | FGFR1 overexpression confers resistance to fulvestrant ± palbociclib, which was reversed by lucitanib | Nat Commun. 2019 Mar 26;10(1):1373 |
| CAMA1 cells | 2 μM | 6 hours | Inhibited the association of FGFR1 with ERα and reduced ERα-dependent gene transcription | Clin Cancer Res. 2017 Oct 15;23(20):6138-6150 |
| Administration | Dosage | Frequency | Description | References | ||
| Nude mice | MCF-7FGFR1 xenograft model | Oral | 10 mg/kg/day | Daily until tumor volume assessment | The triple therapy (fulvestrant + palbociclib + lucitanib) significantly inhibited tumor growth in FGFR1-overexpressing tumors, reducing p-RB and p-FGFR1 levels | Nat Commun. 2019 Mar 26;10(1):1373 |
| BALB/c nude mice | SW579 and TT xenograft models | Oral | 5–20 mg·kg-1·d-1 | Once daily for 21 days | AL3810 significantly inhibited tumor growth in SW579 and TT xenograft models and reduced microvessel density in tumor tissues. | Acta Pharmacol Sin. 2017 Nov;38(11):1533-1542 |
| Female NCr-nu/nu mice | Lung, gastric and endometrial carcinoma xenograft models | Oral | 2.5, 5, 10 or 20 mg/kg | Once daily for 30 days | To evaluate the antitumor activity of Lucitanib in FGFR1/2 amplified or mutated tumor models. Results showed dose-dependent tumor growth inhibition in all models, with more significant effects in FGFR1 amplified lung cancer models. | Neoplasia. 2017 Jan;19(1):35-42 |
| Female athymic nude mice | ER+/HER2-/FGFR1-amplified PDX models | Oral | 7 mg/kg/day | Once daily for 3 weeks | Combination of fulvestrant and lucitanib significantly inhibited tumor growth | Clin Cancer Res. 2017 Oct 15;23(20):6138-6150 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.25mL 0.45mL 0.23mL |
11.27mL 2.25mL 1.13mL |
22.55mL 4.51mL 2.25mL |
|
| CAS号 | 1058137-23-7 |
| 分子式 | C26H25N3O4 |
| 分子量 | 443.49 |
| SMILES Code | O=C(NC)C1=CC=CC2=C1C=CC(OC3=CC=NC4=CC(OCC5(N)CC5)=C(OC)C=C43)=C2 |
| MDL No. | MFCD20527751 |
| 别名 | E-3810; Lucitanib hydrochloride; AL3810 |
| 运输 | 蓝冰 |
| InChI Key | CUDVHEFYRIWYQD-UHFFFAOYSA-N |
| Pubchem ID | 25031915 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 20 mg/mL(45.1 mM),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 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
|
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