400-115-0588
在線咨詢CAS 1942114-09-1, EAI045 小分子抑制劑(純度98)
西安瑞禧生物科技有限公司提供各種科研用小分子抑制劑產(chǎn)品。價格便宜治療好。
產(chǎn)品名稱：EAI045
別名：α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-isoindole-2-acetamide
CAS#:1942114-09-1
中文同義詞：2-(5-氟-2-羥基苯基)-2-(1-氧代異吲哚啉-2-基)-N-(噻唑-2-基)乙酰胺;ALPHA-(5-氟-2-羥基苯基)-1,3-二氫-1-氧代-N-2-噻唑基-2H-異吲哚-2-乙酰胺
結構式：
外觀：白色粉末
純度：98%+
分子式：C19H14FN3O3S
分子量：383.40 Da
存儲條件：-20℃
保存時間：1年
廠家：西安瑞禧生物科技有限公司
該類產(chǎn)品僅僅用于科研，不能用于治療、藥物開發(fā)、和其他商業(yè)用途。
實驗推薦：
EAI045和愛必妥聯(lián)合：小鼠模型中，接近80%
1.用于一代藥物耐藥，有T790M突變的病人對于這類病人，蘿卜上文已經(jīng)提到，已經(jīng)有神藥AZD9291可以吃了，但這個新藥和愛必妥連用，似乎也挺好，在小鼠模型中，高達80%左右(圖中紅色的就是兩藥聯(lián)合的病鼠，柱子朝下就代表腫瘤縮小，縱坐標的數(shù)字代表腫瘤縮小的比例)。
2. 用于吃AZD9291耐藥，有C797S突變的病人
已經(jīng)有AZD9291了，很多病人并不關心上面兩張圖，但這張圖一定得好好看：這是吃了AZD9291耐藥的病人，如果有C797S突變，這個新藥和愛必妥連用，在小鼠模型中，高達80%(5只老鼠，4只有效)。
EAI045 potently inhibits EGFR Y1173phosphorylation in H1975 cells (EC50=2 nM), but not in HaCaT cells. EAI045 isan inhibitor of the L858R/T790M mutant with 1000-fold selectivity versus wildtype EGFR at 1 mM ATP. Profiling of EAI045 against a panel of 250 proteinkinases reveals exquisite selectivity; no other kinases are inhibited by morethan 20% at 1 μM EAI045[1]. EAI045 has high potency and selectivity forL858R/T790M mutation. In L858R/T790M-mutant NSCLC cell line H1975 cells, EAI045decreases but does not completely abolish the EGFR autophosphorylation. Instably transfected NIH-3T3 cells harboring the L858R/T790M EGFR mutant, EAI045shows the same activity. In L858R-mutant H3255 cells, EAI045 exhibits moderateactivity. In the HaCaT cells, a keratinocyte cell line with wild-type EGFR,EAI045 does not show any activity of inhibiting EGFR phosphorylation. Itconfirms the selectivity of EAI045 for mutant EGFRb
In a genetically engineered mouse model ofL858R/T790Mmutant-driven lung cancer , remarkable tumor regression is observedin L858R/T790M-mutant mice treated with the combination of EAI045 andcetuximab. No response is seen in those mice treated with EAI045 alone. Thesame effect is seen in both L858R/T790M/C797S- engineered Ba/F3 cells and inmice carrying the L858R/T790M/C797S tumor xenografts. These assays clearly showthat EAI045 can overcome resistance from acquired T790M and C797S mutation
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LGX818 1269440-17-6
Degarelix 214766-78-6
Irinotecan hydrochloride 100286-90-6
Salinomycin sodium salt 55721-31-8
AGI-5198 1355326-35-0
PHA-665752 477575-56-7
Bafetinib 859212-16-1
Abiraterone 154229-19-3
Calyculin A 101932-71-2
Dovitinib 405169-16-6
Epothilone D 189453-10-9
Homoharringtonine 26833-87-4
Dorsomorphin 866405-64-3
Tamibarotene 94497-51-5
Berberine chloride hydrate 141433-60-5
Puromycin aminonucleoside 58-60-6
Daun02 290304-24-4
Epoxomicin 134381-21-8
Adarotene 496868-77-0
Nobiletin 478-01-3
Idarubicin hydrochloride 57852-57-0
ASC-J9 52328-98-0
Retaspimycin hydrochloride 857402-63-2
Marimastat 154039-60-8
CMK 821794-90-5
Vinblastine 865-21-4
A-366 1527503-11-2
Deforolimus 572924-54-0
DMXAA 117570-53-3
Elesclomol 488832-69-5
Levomefolic acid 31690-09-2
Parthenolide 20554-84-1
Kaempferol 520-18-3
GSK2256098 1224887-10-8
XCT-790 725247-18-7
Bestatin 58970-76-6
Raltitrexed 112887-68-0
Flutamide 13311-84-7
Thalidomide 50-35-1
Trifluorothymidine 70-00-8
Bax inhibitor peptide V5 579492-81-2
LY2606368 dihydrochloride 1234015-54-3
Lapatinib ditosylate 388082-77-7
Isoliquiritigenin 961-29-5
Epothilone B 152044-54-7
Cabazitaxel 183133-96-2
Dacinostat 404951-53-7
Luteolin 木樨草素 491-70-3
SGC0946 1561178-17-3
Eribulin mesylate 441045-17-6
Importazole 662163-81-7
Teniposide 29767-20-2
Tubastatin A Hydrochloride 1310693-92-5
Paradol 27113-22-0
Danusertib 827318-97-8
Deguelin 522-17-8
Pyridostatin hydrochloride 1781882-65-2
Silibinin 22888-70-6
Pralatrexate(Folotyn) 146464-95-1
Bazedoxifene acetate 198481-33-3
Sitravatinib 1123837-84-2
Sitravatinib 1123837-84-2
Kenpaullone 142273-20-9
Harringtonine 26833-85-2
FH535 108409-83-2
Reversine 656820-32-5
Astragaloside IV 84687-43-4
ML364 1991986-30-1
Procyanidin B2 29106-49-8
Lonafarnib 193275-84-2
TGX-221 663619-89-4
PAC-1 315183-21-2
Thiazovivin 1226056-71-8
AZD1152 722543-31-9
SJG-136 232931-57-6
MC1568 852475-26-4
Cyclophosphamide 6055-19-2
Pirarubicin Hydrochloride 95343-20-7
Sapitinib 848942-61-0
Anlotinib 1058156-90-3
Emodin 518-82-1
蟾毒靈(Bufalin) 465-21-4
Isotretinoin(13-cis-Retinoic acid) 4759-48-2
Ixabepilone 219989-84-1
Nelarabine 121032-29-9
Rogaratinib 1443530-05-9
863971-53-3
PD 150606 179528-45-1
Scriptaid 287383-59-9
Anamorelin 249921-19-5
Betulinic acid 472-15-1
N-Desethyl Sunitinib 356068-97-8
TOK-001 851983-85-2
AZD-2461 1174043-16-3
Ezatiostat 168682-53-9
Valrubicin 56124-62-0
Nexturastat A 1403783-31-2
Temoporfin(KW 2345) 122341-38-2
Citarinostat 1316215-12-9
Val-cit-PAB-OH 159857-79-1
β-Lapachone 4707-32-8
Embelin 550-24-3
MMAD 203849-91-6
Bithionol 97-18-7
Hydroxysafflor yellow A 78281-02-4
Litronesib 910634-41-2
Piperazine erastin 1538593-71-3
Tenovin-1 380315-80-0
脫水淫羊藿素(Icaritin) 118525-40-9
土木香內(nèi)酯(Alantolactone) 546-43-0
千層紙素 (OroxylinA) 480-11-5
Pyrotinib (SHR-1258) 1269662-73-8
Glycyrrhizic acid 1405-86-3
Heparan sulfate 9050-30-0
PP121 1092788-83-4
Voreloxin Hydrochloride 175519-16-1
Mitapivat 1260075-17-9
Indirubin 479-41-4
Tenalisib 1639417-53-0
| 序號 | 新聞標題 | 瀏覽次數(shù) | 作者 | 發(fā)布時間 |
|---|---|---|---|---|
| 1 | DOPC Liposome包載CY5脂質(zhì)體包載CY菁染料定制 | 935 | 瑞禧生物 | 2022-10-31 |
| 2 | 水溶性PEG連接劑Azido-PEG6-acid；N3-PEG6-COOH用于生物偶聯(lián) | 765 | 瑞禧生物 | 2023-01-03 |
| 3 | 可降解6 個單元 PEG 的 ADC linker之Azido-PEG6-NHS ester瑞禧生物 | 841 | 瑞禧生物 | 2023-01-03 |
| 4 | 瑞禧生物Azido-PEG7-amine；N3-PEG7-NH2疊氮PEG7氨基 | 731 | 瑞禧生物 | 2023-01-03 |
| 5 | 瑞禧ROS響應性定制： DSPE-TK-PEO ；DBCO-SS-COOH/MAL科研 | 1094 | 瑞禧生物 | 2022-12-08 |
| 6 | 2022瑞禧 生物素化響應性Biotin-PEG-SS-DBCO/Biotin-SS-Sulfo-NHS | 768 | 瑞禧生物 | 2022-12-08 |
| 7 | 2022瑞禧 可選分子量 PCL-TK-PEI-DOX/FA 聚已內(nèi)酯響應性 | 883 | 瑞禧生物 | 2022-12-08 |
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