货号:A100327
同义名:
EXEL-7647; XL647
XL647 or tesevatinib inhibits EGFR, HER2, VEGFR and EphB4 with potential antineoplastic activity.


| 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 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解

| 产品名称 | EGFR/ErbB1 ↓ ↑ | ErbB3 ↓ ↑ | ErbB4 ↓ ↑ | HER2/ErbB2 ↓ ↑ | mutant EGFR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| WZ-3146 |
++++
EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM |
99%+ | |||||||||||||||||
| Daphnetin |
+
EGFR, IC50: 7.67 μM |
PKA,PKC | 95% | ||||||||||||||||
| Lifirafenib |
++
EGFR, IC50: 29 nM |
+
EGFR(T790M/L858R), IC50: 495 nM |
98% | ||||||||||||||||
| PD168393 |
++++
EGFR, IC50: 0.70 nM |
99%+ | |||||||||||||||||
| Nazartinib |
++
mutant EGFR, Ki: 0.031 μM |
++
mutant EGFR, Ki: 0.031 μM |
98% | ||||||||||||||||
| Norcantharidin | ✔ | 98% | |||||||||||||||||
| CL-387785 |
++++
EGFR, IC50: 370 pM |
98% | |||||||||||||||||
| WHI-P154 |
+++
EGFR, IC50: 4 nM |
Src,VEGFR | 98% | ||||||||||||||||
| Tyrphostin A9 |
+
EGFR, IC50: 460 μM |
PDGFR | 98% | ||||||||||||||||
| AG 555 |
+
EGFR, IC50: 0.7 μM |
98% | |||||||||||||||||
| AG 494 |
+
EGFR, IC50: 1.2 μM |
99%+ | |||||||||||||||||
| AG-556 |
+
EGFR, IC50: 5 μM |
98% | |||||||||||||||||
| RG13022 |
+
EGFR, IC50: 4 μM |
99%+ | |||||||||||||||||
| Tyrphostin RG 14620 | ✔ | 99%+ | |||||||||||||||||
| Vandetanib |
+
EGFR, IC50: 500 nM |
99% | |||||||||||||||||
| CNX-2006 |
++
mutant EGFR, IC50: <20 nM |
++
mutant EGFR, IC50: <20 nM |
99% | ||||||||||||||||
| AZD3759 |
++++
EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM |
98% | |||||||||||||||||
| Erlotinib |
++++
EGFR, IC50: 2 nM |
95% | |||||||||||||||||
| Saracatinib |
+++
EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM |
99%+ | |||||||||||||||||
| AG1557 | ✔ | 99% | |||||||||||||||||
| Rociletinib |
++
EGFR (wt), Ki: 303.3 nM EGFR (L858R/T790M), Ki: 21.5 nM |
98% | |||||||||||||||||
| AG490 |
+
EGFR, IC50: 0.1 μM |
98% | |||||||||||||||||
| Cetuximab |
++++
EGFR, Kd: 0.39 nM |
95% | |||||||||||||||||
| Osimertinib |
++
L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 nM |
98% | |||||||||||||||||
| Osimertinib mesylate | ✔ | 98% (Content MsOH 15.2-18.2%) | |||||||||||||||||
| Chrysophanol | ✔ | mTOR | 98% | ||||||||||||||||
| PD153035 |
++++
EGFR, Ki: 5.2 pM |
99%+ | |||||||||||||||||
| Olmutinib | ✔ | BTK | 99%+ | ||||||||||||||||
| WZ4002 |
++++
EGFR (L858R), IC50: 2 nM EGFR (L858R/T790M), IC50: 8 nM |
99%+ | |||||||||||||||||
| Icotinib |
+++
EGFR, IC50: 5 nM |
99% | |||||||||||||||||
| Desmethyl Erlotinib HCl |
++++
EGFR, IC50: 2 nM |
98% | |||||||||||||||||
| Cyasterone | ✔ | 99%+ | |||||||||||||||||
| PP 3 |
+
EGFR tyrosine kinase, IC50: 2.7 μM |
98% | |||||||||||||||||
| WZ8040 | ✔ | 99%+ | |||||||||||||||||
| (-)-Epigallocatechin Gallate | ✔ | 99% | |||||||||||||||||
| AG 18 |
+
EGFR, IC50: 35 μM |
99%+ | |||||||||||||||||
| O-Desmethyl gefitinib |
++
EGFR, IC50: 36 nM |
99% | |||||||||||||||||
| Falnidamol | ✔ | 99%+ | |||||||||||||||||
| AZ-5104 |
++++
EGFR (L861Q) , IC50: <1 nM EGFR (L858R), IC50: 6 nM |
+++
ErbB4, IC50: 7 nM |
BRK | 99%+ | |||||||||||||||
| Butein | ✔ | 95% | |||||||||||||||||
| Genistein | ✔ | 98% | |||||||||||||||||
| SU5214 |
+
EGFR, IC50: 36.7 μM |
99%+ | |||||||||||||||||
| Naquotinib | ✔ | 99%+ | |||||||||||||||||
| Gefitinib |
++
EGFR, IC50: 15.5 nM |
+
EGFR (858R/T790M), IC50: 823.3 nM |
98% | ||||||||||||||||
| Theliatinib |
+++
WT EGFR, IC50: 3 nM |
++
EGFR T790M/L858R, IC50: 22 nM |
99% | ||||||||||||||||
| Lazertinib |
++++
L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 nM |
++++
Del19/T790M, IC50: 1.7 nM |
99%+ | ||||||||||||||||
| Gefitinib-based PROTAC 3 |
++
EGFR, DC50: 22.3 nM |
99%+ | |||||||||||||||||
| MTX-211 | ✔ | PI3K | 98% | ||||||||||||||||
| (E)-AG 99 | ✔ | 99%+ | |||||||||||||||||
| Licochalcone D | ✔ | PARP,Caspase | 99% | ||||||||||||||||
| Zipalertinib |
+++
EGFR (L861Q), IC50: 4.1 nM EGFR WT, IC50: 8 nM |
+++
HER4, IC50: 4 nM |
++++
EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM |
97% | |||||||||||||||
| JND3229 |
+++
EGFR WT, IC50: 6.8 nM |
++
EGFR L858R/T790M, IC50: 30.5 nM |
99%+ | ||||||||||||||||
| Firmonertinib mesylate | ✔ | 99%+ | |||||||||||||||||
| Tyrphostin AG30 | ✔ | 99%+ | |||||||||||||||||
| EGFR-IN-12 |
++
EGFR, IC50: 21 nM |
99%+ | |||||||||||||||||
| Mobocertinib | ✔ | 98% | |||||||||||||||||
| (Rac)-JBJ-04-125-02 | ✔ | 95% | |||||||||||||||||
| (S)-Sunvozertinib | ✔ | 99% | |||||||||||||||||
| BLU-945 | ✔ | 95% | |||||||||||||||||
| Poziotinib |
+++
HER1, IC50: 3.2 nM |
++
HER4, IC50: 23.5 nM |
+++
HER2, IC50: 5.3 nM |
98% | |||||||||||||||
| TAK-285 |
++
EGFR/HER1, IC50: 23 nM |
+
HER4, IC50: 260 nM |
++
HER2, IC50: 17 nM |
99%+ | |||||||||||||||
| ARRY-380 analog | ✔ | 99% | |||||||||||||||||
| Canertinib |
++++
EGFR, IC50: 1.5 nM |
+++
ErbB2, IC50: 9.0 nM |
99%+ | ||||||||||||||||
| Dacomitinib |
+++
EGFR, IC50: 6.0 nM |
+
ErbB4, IC50: 73.7 nM |
+
ErbB2, IC50: 45.7 nM |
98% | |||||||||||||||
| EGFR/ErbB-2/ErbB-4 inhibitor-2 |
+
ErbB4, IC50: 1.91 μM |
+
ErbB2, IC50: 0.08 μM |
99%+ | ||||||||||||||||
| (E/Z)-CP-724714 |
++
HER2/ErbB2, IC50: 10 nM |
95% | |||||||||||||||||
| Lapatinib |
++
EGFR, IC50: 10.8 nM |
+
ErbB4, IC50: 367 nM |
+++
ErbB2, IC50: 9.2 nM |
98% | |||||||||||||||
| AEE788 |
++++
EGFR, IC50: 2 nM |
+
HER4/ErbB4, IC50: 160 nM |
+++
HER2/ErbB2, IC50: 6 nM |
c-Fms/CSF1R | 98+% | ||||||||||||||
| AV-412 free base |
++++
EGFR, IC50: 0.75 nM |
++
ErbB2, IC50: 19 nM |
++++
EGFRL858R/T790M, IC50: 0.51 nM EGFRT790M, IC50: 0.79 nM |
98+% | |||||||||||||||
| Neratinib |
+
EGFR, IC50: 92 nM |
+
HER2, IC50: 59 nM |
Src | 98% | |||||||||||||||
| BMS-599626 |
++
HER1, IC50: 20 nM |
+
HER4, IC50: 190 nM |
++
HER2, IC50: 30 nM |
98% | |||||||||||||||
| Tucatinib |
+++
ErbB2, IC50: 8 nM |
98% | |||||||||||||||||
| Allitinib |
++++
EGFR, IC50: 0.5 nM |
++++
ErbB4, IC50: 0.8 nM |
+++
ErbB2, IC50: 3.0 nM |
99% | |||||||||||||||
| Pelitinib |
+
EGFR, IC50: 38.5 nM |
+
ErbB2, IC50: 1.255 μM |
Raf,Src | 99%+ | |||||||||||||||
| Sapitinib |
+++
EGFR, IC50: 4 nM |
+++
ErbB3, IC50: 4 nM |
+++
ErbB2, IC50: 3 nM |
99%+ | |||||||||||||||
| CUDC-101 |
+++
EGFR, IC50: 2.4 nM |
++
HER2, IC50: 15.7 nM |
HDAC | 99%+ | |||||||||||||||
| Varlitinib |
+++
ErbB1, IC50: 7 nM |
++++
ErbB2, IC50: 2 nM |
99%+ | ||||||||||||||||
| Afatinib dimaleate |
++++
EGFR (wt), IC50: 0.5 nM EGFR (L858R/T790M), IC50: 0.4 nM |
++
HER2, IC50: 14 nM |
98% | ||||||||||||||||
| Canertinib 2HCl |
+++
EGFR, IC50: 7.4 nM |
+++
ErbB2, IC50: 9 nM |
99% | ||||||||||||||||
| Allitinib tosylate |
++++
EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 nM |
++++
ErbB4, IC50: 0.8 nM |
+++
ErbB2, IC50: 3.0 nM |
99% | |||||||||||||||
| Tyrphostin AG 528 |
+
EGFR, IC50: 4.9 μM |
+
HER2, IC50: 2.1 μM |
97% | ||||||||||||||||
| Afatinib |
++++
EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM |
++++
ErbB4, IC50: 1 nM |
++
HER2, IC50: 14 nM |
99% | |||||||||||||||
| Pyrotinib dimaleate |
++
EGFR, IC50: 0.013 μM |
++
HER2, IC50: 0.038 μM |
98% | ||||||||||||||||
| Epertinib HCl |
++++
EGFR, IC50: 1.48 nM |
+++
HER4, IC50: 2.49 nM |
+++
HER2, IC50: 7.15 nM |
99% | |||||||||||||||
| Tuxobertinib |
++++
EGFR, Kd: 0.2 nM |
++++
HER2, Kd: 0.76 nM |
99% | ||||||||||||||||
| ALK-IN-1 |
++
EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM |
ALK | 99% | ||||||||||||||||
| Brigatinib |
+
EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 nM |
ALK,FLT3 | 98% | ||||||||||||||||
| Avitinib |
++++
EGFR L858R/T790M, IC50: 0.18 nM |
BTK | 99%+ | ||||||||||||||||
| EAI045 | ✔ | 97% | |||||||||||||||||
| Almonertinib | ✔ | 99% | |||||||||||||||||
| BI-4020 |
++++
EGFRdel19 T790M C797S, IC50: 0.2 nM |
99%+ | |||||||||||||||||
| EGFR-IN-7 |
++++
EGFRL858R/T790M, IC50: 0.19 nM EGFRd746-750/T790M/C797S, IC50: 0.26 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 | HER2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Poziotinib |
++++
HER2, IC50: 5.3 nM |
98% | |||||||||||||||||
| Tyrphostin AG 879 |
+
HER2-Neu, IC50: 1.0 μM |
95% | |||||||||||||||||
| TAK-285 |
+
HER2, IC50: 17 nM |
99%+ | |||||||||||||||||
| ARRY-380 analog | ✔ | 99% | |||||||||||||||||
| Canertinib |
+++
ErbB2, IC50: 9.0 nM |
EGFR | 99%+ | ||||||||||||||||
| (E/Z)-CP-724714 |
++
HER2/ErbB2, IC50: 10 nM |
95% | |||||||||||||||||
| Lapatinib |
+++
ErbB2, IC50: 9.2 nM |
EGFR | 98% | ||||||||||||||||
| AEE788 |
++++
HER2/ErbB2, IC50: 6 nM |
EGFR | 98+% | ||||||||||||||||
| Neratinib |
+
HER2, IC50: 59 nM |
Src,EGFR | 98% | ||||||||||||||||
| BMS-599626 |
+
HER2, IC50: 30 nM |
98% | |||||||||||||||||
| Mubritinib |
++++
HER2/ErbB2, IC50: 6.0 nM |
99%+ | |||||||||||||||||
| Tucatinib |
+++
ErbB2, IC50: 8 nM |
98% | |||||||||||||||||
| Sapitinib |
++++
ErbB2, IC50: 3 nM |
EGFR | 99%+ | ||||||||||||||||
| CUDC-101 |
++
HER2, IC50: 15.7 nM |
EGFR,HDAC | 99%+ | ||||||||||||||||
| Afatinib dimaleate |
++
HER2, IC50: 14 nM |
98% | |||||||||||||||||
| Afatinib |
++
HER2, IC50: 14 nM |
99% | |||||||||||||||||
| Pertuzumab | ✔ | 95% | |||||||||||||||||
| Trastuzumab | ✔ | 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 |
PDGFR,c-Kit,FGFR | 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 |
c-Kit,FLT3 | 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/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM |
+
VEGFR3/FLT4, IC50: 660 nM |
c-Fms/CSF1R,c-Kit | 99%+ | ||||||||||||||
| Axitinib |
++++
VEGFR1/FLT1, IC50: 0.1 nM |
++++
VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM |
98% | ||||||||||||||||
| Dovitinib |
+++
VEGFR1/FLT1, IC50: 10 nM |
+++
VEGFR2/Flk1, IC50: 13 nM |
+++
VEGFR3/FLT4, IC50: 8 nM |
c-Kit,FLT3 | 99%+ | ||||||||||||||
| ZM 306416 |
+
VEGFR1, IC50: 0.33 μM |
Src | 99%+ | ||||||||||||||||
| KRN-633 |
+
VEGFR1, IC50: 170 nM |
+
VEGFR2, IC50: 160 nM |
+
VEGFR3, IC50: 125 nM |
c-Kit,BTK | 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 |
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。 | |||||||||||||||||||
| 描述 | XL647 is a selective EGFR inhibitor with IC50 values of 0.3nM, 16nM, 1.5nM, 8.7nM and 1.4nM for EGFR, ErbB2, KDR, Flt-4 and EphB4, respectively. XL647 inhibited cellular WT and mutant EGFR phosphorylation with IC50 values of 1nM, 12nM, 5nM, 10nM, 5nM and 74nM for EGFR WT (A431), EGFR WT (pCMV/Lx-1), EGFR L858R (pCMV/Lx-1), EGFR L861Q (pCMV/Lx-1), EGFR WT (pTet-On/Lx-1) and EGFR Variant III (pTet-On/Lx-1), respectively. It inhibitsed cellular proliferation and EGFR pathway activation, including p-AKT and p-ERK, in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. Oral administration of XL647 at doses of 10mg/kg, 30mg/kg and 100mg/kg, once daily for 28 days, dose-dependently inhibited tumor growth in athymic mice xenograft A431 tumors. Similarly, significant tumor growth inhibition by administration of XL647 at dose of 100mg/kg could be observed in severe combined immunodeficient mice subcutaneously implantated with H1975 tumor and nude mice subcutaneously implantated with MDA-MB-231 tumor in mammary fat pad. In vivo efficacy studies showed that XL647 reduced both tumor EGFR signaling and tumor vessel density[2]. |
| 作用机制 | XL647 is a reversible and ATP competitive inhibitor.[2] |
| Concentration | Treated Time | Description | References | |
| GBM12 | 0–1000 nM | 14 days | Assess cell viability, IC50 of 11 nmol/L | Mol Cancer Ther. 2021 Jun;20(6):1009-1018 |
| GBM6 | 0–1000 nM | 18 days | Assess cell viability, IC50 of 102 nmol/L | Mol Cancer Ther. 2021 Jun;20(6):1009-1018 |
| GBM108, GBM76, GBM39, GBM84, GBM08 | 0–10,000 nM | 6 to 9 days | Assess cell viability, EGFRvIII mutant models showed reduced sensitivity to tesevatinib and erlotinib | Mol Cancer Ther. 2021 Jun;20(6):1009-1018 |
| Administration | Dosage | Frequency | Description | References | ||
| FVB wild-type mice and FVB Mdr1a/b(−/−)Bcrp1(−/−) triple knockout mice | Non-tumor bearing mouse model | Oral or intraperitoneal infusion | 70 mg/kg oral or 10 mg/mL intraperitoneal infusion | Single dose or 48-hour continuous infusion | Assess tesevatinib distribution in brain and plasma, brain concentrations in WT and TKO mice were 0.72 and 10.03 μg/g, respectively | Mol Cancer Ther. 2021 Jun;20(6):1009-1018 |
| Dose | Mice: 7.5 mg/kg , 15 mg/kg[2] (i.p.); 100 mg/kg[1] (p.o.) |
| Administration | i.p., p.o. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.18mL 2.04mL 1.02mL |
20.35mL 4.07mL 2.04mL |
|
| CAS号 | 781613-23-8 |
| 分子式 | C24H25Cl2FN4O2 |
| 分子量 | 491.39 |
| SMILES Code | CN1C[C@@]2([H])[C@@](C[C@@H](COC3=CC4=NC=NC(NC5=CC=C(Cl)C(Cl)=C5F)=C4C=C3OC)C2)([H])C1 |
| MDL No. | MFCD22124889 |
| 别名 | EXEL-7647; XL647; KD-019; XL-647 |
| 运输 | 蓝冰 |
| InChI Key | HVXKQKFEHMGHSL-GOOCMWNKSA-N |
| Pubchem ID | 10458325 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(213.68 mM),配合低频超声助溶,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 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
|
沪公网安备 31011702889066号
沪ICP备2024050318号-1