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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品。價格便宜治療好。

產品名稱：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

該類產品僅僅用于科研，不能用于治療、藥物開發、和其他商業用途。

實驗推薦：

EAI045和愛必妥聯合：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，蘿卜上文已經提到，已經有神藥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合的病鼠，柱子朝下就代表腫瘤縮小，縱坐標的數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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Abiraterone Acetate       乙酸阿比特龍酯    154229-18-2

Ifosfamide      異環磷酰胺    3778-73-2

Zalcitabine,DDC    扎西他濱,2',3'-二脫氧胞苷   7481-89-2

Ascomycin,FK520  子囊霉素       104987-12-4;11011-38-4

Calcium levofolinate      左亞葉酸鈣；甲酰四氫葉酸鈣    80433-71-2

23-羥基白樺酸Anemosapogenin         85999-40-2

沙力度銨Thalidomide(Distaval)         50-35-1

硼替佐咪Bortezomib         179324-69-7

門冬酰胺酶Asparaginase            9015-68-3

甲氨喋呤Methotrexate         59-5-2

培美曲塞二鈉(Alimta)         150399-23-8

卡培他濱Capecitabine         154361-50-9

紫杉醇Paclitaxel  270/g             33069-62-4

氟尿嘧啶5-Fluorouracil              51-21-8

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米替福新Miltefosine    Hexadecyl phosphocholine; Hexadecyl2-(trimethylamino)ethyl phosphate       58066-85-6

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丁二酸(琥珀酸)Succinic acid             110-15-6

醋酸卡泊芬凈CasporfunginAcetate           179463-17-3

多西紫杉醇 380/g Docetaxel, Taxotere      

10-羥基喜樹堿      10-Hydroxy camptothecin     19685-09-7

氟維司群      Fulvestrant     129453-61-8

吡柔比星             

米托蒽醌             

長春瑞濱             

拓撲替康             

伊立替康             

甲磺酸伊馬替尼    Imatinib  220127-57-1

吉非替尼       Gefitinib        184475-35-2

達沙替尼       Dasatinib 863127-77-9

尼羅替尼       Nilotinib 641571-10-0

凡德他尼       Vandetanib     443913-73-3

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阿西替尼       Axitinib  319460-85-0

依維莫司       Everolimus     159351-69-6

替莫唑胺       Temozolomid        85622-93-1

來那替尼       Neratinib       698387-09-6

博舒替尼       Bosutinib 380843-75-4

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西地尼布       cediranib 379231-04-6

克里唑蒂尼    Crizotinib      877399-52-5

莫立替尼, 木利替尼    Mubritinib    366017-09-6

奧拉帕尼       Olaparid  763113-22-0

陶扎色替       Tozasertib       639089-54-6

       Ruxolitinib     941678-49-5

       AmuvatinibMP-470      850879-09-3

       LenvatinibE7080   417716-92-8

       Motesanib(AMG706)     453562-69-1， 857876-30-3

多韋替尼       Dovitinib TKI-258 915769-50-5，852433-84-2

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硼替佐米       Bortezomib     179324-69-7

布立尼布       Brivanib alaninate  649735-63-7

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       Ponatinib      943319-70-8

       Linifanib 796967-16-3

西地尼布       recentin   288383-20-0

依維莫司       everolimus      159351-69-6

伊馬替尼       Imatinib  152459-95-5

阿那曲唑       Anastrozole    120511-73-1

2-甲氧基雌二醇    2-Methoxyestradiol 362-07-2

2-巰基乙烷磺酸鈉 Mesna     19767-45-4

              1256580-46-7

Tivozanib, AV951          475108-18-0

BGJ398(NVP-BGJ398)        872511-34-7

卡莫司汀/卡氮芥          154-93-8

INCB018424) phosphate              1092939-17-7

SB-431542            301836-41-9

Tariquidar,XR-9576              206873-63-4

Afatinib/BIBW2992             439081-18-2

Epothilone B (EPO906, Patupilone)            152044-54-7

              186692-73-9

AICAR   2627-69-2    

XMU-MP-1    2061980-01-4     

Erastin    571203-78-6  

Y-27632  146986-50-7

MK-4827       1038915-60-4

XAV-939 284028-89-3

PT-2385  1672665-49-4

Vorinostat       149647-78-9  

SCH772984    942183-80-4  

5-Azacytidine         320-67-2     

CB-839   1439399-58-2

Decitabine      2353-33-5    

Panobinostat   404950-80-7  

DMOG    89464-63-1  

R428       1037624-75-1

Regorafenib    755037-03-7

PD0325901    391210-10-9  

OTX-015 202590-98-5  

TEPP-46       1221186-53-3

BYL-719 1217486-61-7

Selumetinib    606143-52-6

SB 202190     152121-30-7  

Nigericin sodium salt    28643-80-3    

Pexidartinib    1029044-16-3

INK-128 1224844-38-5

Mdivi-1   338967-87-6  

Nocodazole     31430-18-9  

Palbociclib hydrochloride      827022-32-2  

alpha-Amanitin      23109-05-9  

GW9662 22978-25-2  

MK-1775       955365-80-7  

Afatinib 850140-72-6  

Etoposide      33419-42-0    

LEE011   1211441-98-3

Docetaxel      114977-28-5  

Dinaciclib       779353-01-4

BIBF 1120      656247-17-5

A 83-01   909910-43-6  

Dabrafenib     1195765-45-7

17-AAG  75747-14-7  

Sorafenib tosylate   475207-59-1  

NVP-BKM120       944396-07-0  

Salinomycin   53003-10-4  

S63845   1799633-27-4

Calcitriol       32222-06-3    

LY2157299     700874-72-2

SU5416   204005-46-9  

Retinoic acid 302-79-4

Silvestrol       697235-38-4  

ICG-001  847591-62-2

Rapamycin     53123-88-9  

MG-132  133407-82-6  

LY294002      154447-36-6

Z-VAD(OMe)-FMK       187389-52-2

(+)-JQ-1 1268524-70-4

Actinomycin D      50-76-0

U0126     1173097-76-1      

MLN4924       905579-51-3

Enzalutamide  915087-33-1

Mitomycin C  1950-7-7

Y-27632 dihydrochloride       129830-38-2

ABT-199 1257044-40-8

SB-431542     301836-41-9  

Dorsomorphin dihydrochloride     1219168-18-9

CHIR-99021   252917-06-9  

AZD-9291      1421373-65-0

Staurosporine  62996-74-1    

MK 2206 dihydrochloride     1032350-13-2

LY2835219     1231930-82-7

Necrostatin-1  4311-88-0    

PD98059 167869-21-8

Trichostatin A         58880-19-6  

Navitoclax      923564-51-6  

Dasatinib 302962-49-8  

Tamoxifen      10540-29-1  

Palbociclib     571190-30-2  

GSK126  1346574-57-9     

BMN-673       1207456-01-6

EPZ-6438       1403254-99-8

Wortmannin    19545-26-7    

AICAR   2627-69-2    

XMU-MP-1    2061980-01-4     

Erastin    571203-78-6  

Y-27632  146986-50-7

MK-4827       1038915-60-4

XAV-939 284028-89-3

PT-2385  1672665-49-4

Vorinostat       149647-78-9  

SCH772984    942183-80-4  

5-Azacytidine         320-67-2     

CB-839   1439399-58-2

Decitabine      2353-33-5    

Panobinostat   404950-80-7  

DMOG    89464-63-1  

R428       1037624-75-1

Regorafenib    755037-03-7

PD0325901    391210-10-9  

OTX-015 202590-98-5  

TEPP-46       1221186-53-3

BYL-719 1217486-61-7

Selumetinib    606143-52-6

SB 202190     152121-30-7  

Nigericin sodium salt    28643-80-3    

Pexidartinib    1029044-16-3

INK-128 1224844-38-5

Mdivi-1   338967-87-6  

Nocodazole     31430-18-9  

Palbociclib hydrochloride      827022-32-2  

alpha-Amanitin      23109-05-9  

GW9662 22978-25-2  

MK-1775       955365-80-7  

Afatinib 850140-72-6  

Etoposide      33419-42-0    

LEE011   1211441-98-3

Docetaxel      114977-28-5  

Dinaciclib       779353-01-4

BIBF 1120      656247-17-5

A 83-01   909910-43-6  

Dabrafenib     1195765-45-7

17-AAG  75747-14-7  

Sorafenib tosylate   475207-59-1  

NVP-BKM120       944396-07-0  

Salinomycin   53003-10-4  

S63845   1799633-27-4

Calcitriol       32222-06-3    

LY2157299     700874-72-2

SU5416   204005-46-9  

Retinoic acid 302-79-4

Silvestrol       697235-38-4  

ICG-001  847591-62-2

Alisertib  1028486-01-2

THZ1      1604810-83-4

ML385    846557-71-9

Streptozocin   18883-66-4    

Lenalidomide  191732-72-6  

Emricasan      254750-02-2  

Carfilzomib    868540-17-4

Monomethyl auristatin E       474645-27-7

Cobimetinib    934660-93-2  

FCCP     370-86-5

AP1903 195514-63-7  

Cilengitide      188968-51-6

Gemcitabine hydrochloride    122111-03-9  

Palbociclib isethionate   827022-33-3

Vincristine sulfate   2068-78-2     

Acalabrutinib        1420477-60-6

Cytarabine      147-94-4     

Z-DEVD-FMK      210344-95-9  

Brigatinib       1197953-54-0      

Torin 1    1222998-36-8

GANT 61      500579-04-4  

Roscovitine     186692-46-6

Birinapant      1260251-31-7

GSK2795039  1415925-18-6

SC79      305834-79-1  

LY2606368     1234015-52-1

Pifithrin-α hydrobromide      63208-82-2  

Cyclophosphamide 50-18-0  

Entinostat       209783-80-2

Ganetespib     888216-25-9  

GDC-0994     1453848-26-4

INNO-206      1361644-26-9     

       1448671-31-5

AZD-8055      1009298-09-2

        4449-51-8    

Bleomycin sulfate   9041-93-4    

GSK 525762A       1260907-17-2     

Triptolide       38748-32-2  

Ko 143    461054-93-3

Methotrexate  59-05-2

GSK343         1346704-33-3     

SAR405         1523406-39-4     

Volasertib       755038-65-4

ALW-II-41-27 1186206-79-0

        755038-02-9

Nutlin 3a 675576-98-4

Quizartinib    950769-58-1

LY2109761    700874-71-1

PF-06463922        1454846-35-5

Gilteritinib      1254053-43-4

UK-5099 56396-35-1

Erlotinib hydrochloride  183319-69-9

        646502-53-6

        128517-07-7

BPTES   314045-39-1

Capsazepine   138977-28-3

BLZ945 953769-46-5

BMS-202       1675203-84-5

Colchicine      64-86-8

Suramin sodium salt      129-46-4

Linsitinib 867160-71-2

Mertansine      139504-50-0

Troglitazone   97322-87-7

Entrectinib     1108743-60-7

Curcumin       458-37-7

Talabostat mesylate 150080-09-4

Veliparib 912444-00-9

Stattic    19983-44-9

PND-1186     1061353-68-1

LOXO-101     1223403-58-4

LDN193189    1062368-24-4

Genistein 446-72-0

Geldanamycin        30562-34-6

BX795    702675-74-9

Sunitinib Malate     341031-54-7

NSC 74859    501919-59-1

Salubrinal       405060-95-9

Campathecin   7689-03-4

VO-Ohpic trihydrate      476310-60-8

A-485     1889279-16-6

Enasidenib      1446502-11-9

YM-155         781661-94-7

Quercetin        117-39-5

Pemetrexed disodium     150399-23-8

Bardoxolone methyl      218600-53-4

UNC1999       1431612-23-5

ARV-825 1818885-28-7

LY2228820    862507-23-1

Elacridar 143664-11-3

JPH203   1037592-40-7

Selonsertib     1448428-04-3

Pazopanib       444731-52-6

Calicheamicin       108212-75-5

Apatinib         1218779-75-9

Belinostat      866323-14-0

RepSox   446859-33-2

Sodium Butyrate    156-54-7

Defactinib       1073154-85-4

Cryptotanshinone   35825-57-1

16頁開始     

Epirubicin hydrochloride      56390-09-1

L-NAME hydrochloride 51298-62-5

Pentostatin      53910-25-1

GSK-J4 1373423-53-0

Bicalutamide   90357-06-5

Ferrostatin-1   347174-05-4

Flavopiridol   146426-40-6

Topotecan Hydrochloride      119413-54-6

Pomalidomide 19171-19-8

Napabucasin   83280-65-3

Honokiol 35354-74-6

Mivebresib     1445993-26-9

SKF-96365     130495-35-1

Exatecan Mesylate  169869-90-3

Tauroursodeoxycholate   35807-85-3

SU 5402         215543-92-3

Epibrassinolide      78821-43-9

Tamoxifen Citrate  54965-24-1

LMI070 (NVS-SM1)    1562338-42-4

CBR-5884     681159-27-3

Shikonin 517-89-5

NADPH  2646-71-1

5-Iodotubercidin    24386-93-4

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