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ResidenceTimer™ キナーゼタンパク質相互作用解析サービス Target List

ResidenceTimer™ はカルナバイオサイエンスのビオチン化キナーゼタンパク質等を用い、SPR(表面プラズモン共鳴)法による化合物とキナーゼ蛋白質の相互作用を速度論的に解析するサービスです。分子間相互作用検出用に開発された高感度SPR機器、Biacore T200 (GE Healthcare)を用いて経時的に観察したアフィニティーセンサーグラムから2分子間の結合特異性を確認、結合親和性をカイネティクス解析致します。

全ターゲットOncolines社で最適化された均一アッセイバッファーにて試験が行われる為ターゲット間のデータ比較が容易です。リストに無いターゲットについてもお気軽にご相談ください。サービスご利用詳細はこちらでご確認ください。

Target Name Pre-profiled therapeutics Sample Data
ABL(ABL1) ponatinib, bosutinib, dasatinib, imatinib
ACVR2A dasatinib
AKT1 GSK690693
AKT2 GSK690693
ALK alectinib, crizotinib
ALK[C1156Y] GSK1838705
ALK[F1174L] crizotinib
ALK[F1174L/G1202R] brigatinib
ALK[G1202R] lorlatinib
ALK[G1269A] brigatinib
ALK[I1171N] brigatinib
ALK[I1171N/L1198F] brigatinib
ALK[I1171S] ceritinib
ALK[I1171T] brigatinib
ALK[L1196M] brigatinib, crizotinib
ALK[L1196M/G1202R] TAE684
ALK[L1198F] gilteritinib
ALK[R1275Q] brigatinib
ALK[V1180L] TAE684
AMPKα1/β1/γ1 GSK690693, WZ4003
AMPKα1/β2/γ1 fasudil, GSK690693, TAE684, WZ4003
AurA (AURKA) MK-5108, pan-Aurora inhibitors
AurB(AURKB)/INCENP * MK-5108, pan-Aurora inhibitors
AXL crizotinib, sunitinib
BMX bosutinib, dasatinib
BRAF dabrafenib, vemurafenib
BRK(PTK6) * ibrutinib
BTK * ponatinib, ibrutinib, dasatinib
BTK[non-activated] ponatinib, ibrutinib, dasatinib
BTK[C481S] * fenebrutinib
BTK[C481S][non-activated] fenebrutinib, ibrutinib
BTK[T316A] * fenebrutinib, ibrutinib
BTK[T316A][non-activated] fenebrutinib, acalabrutinib
BTK[T474I] * ARQ-531, ibrutinib
BTK[T474I][non-activated] ibrutinib
BTK[T474S] * ARQ-531, ibrutinib
BTK[T474S][non-activated] ibrutinib
CaMK2β(CAMK2B) midostaurin
CaMK2δ(CAMK2D) sunitinib
CDK1(CDC2)/CycA2 staurosporine
CDK1(CDC2)/CycB1 AT7519, dinaciclib, flavopiridol, PHA-793887, PHA-848125
CDK2/CycA2 PHA-793887, dinaciclib
CDK2/CycE1 SNS-032
CDK3/CycE1 AT7519
CDK4/CycD1 dinaciclib
CDK4/CycD3 dinaciclib, palbociclib, ribociclib, abemaciclib
CDK5/p25 SNS-032, dinaciclib
CDK6/CycD1 dinaciclib
CDK6/CycD3 ribociclib
CDK6/CycD3[non-activated] ribociclib
CDK7/CycH/MAT1 dinaciclib, pan-CDK inhibitors
CDK8/CycC staurosporine
CDK9/CycK PHA-739887, dinaciclib
CDK9/CycT1 dinaciclib, pan-CDK inhibitors
CDK9/CycT2 staurosporine, dinaciclib
CHK1(CHEK1) bosutinib, sunitinib
DDR1 imatinib
DDR2 * ponatinib, dasatinib, imatinib, sorafenib
EGFR afatinib, erlotinib, gefitinib
EGFR[C797S] afatinib
EGFR[C797S/L858R] afatinib, erlotinib, gefitinib
EGFR[d746-750] gefitinib, erlotinib, afatinib
EGFR[d746-750/C797S] gefitinib, erlotinib, afatinib
EGFR[d746-750/T790M/C797S/L858R] brigatinib
EGFR[L858R] afatinib
EGFR[T790M] afatinib
EGFR[T790M/L858R] osimertinib
EPHA2 BMS-777607, dasatinib, staurosporine,
FAK(PTK2) crizotinib
FGFR1 * infigratinib, ponatinib
FGFR1[non-activated] infigratinib, ponatinib
FGFR2 * ponatinib
FGFR2[non-activated] ponatinib
FGFR2[C491A/V564I] * dovitinib
FGFR2[C491A] * ponatinib
FGFR2[C491A][non-activated] ponatinib
FGFR2[C491A/V564I][non-activated] ponatinib
FGFR2[N549H] * axitinib
FGFR2[N549H][non-activated] axitinib
FGFR2[V564I] * axitinib
FGFR2[V564I][non-activated] axitinib
FGFR2[V564L] * axitinib
FGFR2[V564L][non-activated] axitinib
FGFR3 * infigratinib, sunitinib
FGFR4 infigratinib, sunitinib
FLT3 * imatinib, dasatinib
FLT3[non-activated] crenolanib, gilteritinib, midostaurin, sunitinib
FMS(CSF1R)[non-activated] dasatinib
FMS(CSF1R) * dasatinib
FYN [isoform a] dasatinib, ponatinib, regorafenib
GCN2(EIF2AK4) A-92
GSK3β(GSK3B) abemaciclib, staurosporine
HPK1(MAP4K1) bosutinib
IGF1R * GSK-1838705, staurosporine, cabozantinib
IGF1R[non-activated] brigatinib
IKKα(CHUK) * IKKβ inhibitor
IKKα(CHUK)[inactive mutant] IKKβ inhibitor
INSR * BMS-754807, ceritinib, GSK1838705A, linsitinib, NVP-ADW742
INSR[non-activated] BMS-754807, ceritinib, GSK1838705A, linsitinib, NVP-ADW742
IRAK4 crizotinib, sunitinib
ITK * crizotinib, sunitinib
JAK2 staurosporine
KDR(VEGFR2) vandetanib
KIT * pazopanib, masitinib, staurosporine
LATS2/MOBKL1A staurosporine
LCK ponatinib, regorafenib
LIMK2 dasatinib
LYNa ponatinib, regorafenib, tamatinib
MAP2K1[inactive] crizotinib, dasatinib, trametinib
MAP3K5 staurosporine, bosutinib, sunitinib
MER(MERTK) BMS-777607
MET crizotinib
MET[D1228H] foretinib
MET[D1228N] foretinib
MET[M1250T] MET/RON inhibitor
MET[Y1230C] crizotinib
MET[Y1230H] MET/RON inhibitor
MLK1(MAP3K9) bosunitib, dabrafenib, midostaurin, sunitinib
MLK2(MAP3K10) bosunitib, dabrafenib, midostaurin, sunitinib
MLK3(MAP3K11) bosunitib, dabrafenib, midostaurin, sunitinib
MST2(STK3) midostaurin
MYLK4 dovitinib
Nuak2 staurosporine
p38α(MAPK14) sorafenib, p38 MAPK inhibitors
p38α(MAPK14)[inactive] sorafenib, p38 MAPK inhibitors
PAK4 GSK690693, staurosporine, bosutinib
PAK6 staurosporine
PDGFRα(PDGFRA) * nintedanib, axitinib, crenolanib, gilteritinib
PDGFRα(PDGFRA)[non-activated] nintedanib, axitinib, crenolanib, gilteritinib
PDGFRβ(PDGFRB) * nintedanib, axitinib, crenolanib, gilteritinib
PDGFRβ(PDGFRB)[non-activated] nintedanib, axitinib, crenolanib, gilteritinib
PIK3CA[E542K]/PIK3R1 idelalisib
PIK3CA[E545K]/PIK3R1 idelalisib
PIK3CA[H1047R]/PIK3R1 idelalisib
PIK3CA[P539R]/PIK3R1 idelalisib
PIK3CA[R88Q]/PIK3R1 idelalisib
PIK3CA/PIK3R1 pictilisib, dactolisib
PIK3CB/PIK3R1 apitolisib
PIK3CD/PIK3R1 idelalisib, duvelisib
PIK3CG apitolisib, dactolisib, duvelisib
PIK3CG/PIK3R5 apitolisib, duvelisib
PIKFYVE(PIP5K3) YM201636
PKACα(PRKACA) A-674563
PKCα(PRKCA) A-674563, enzastaurin, sotrastaurin
PKCη(PRKCH) staurosporine
PKN1 GSK690693
PLK1 GSK461364
PYK2(PTK2B) * crizotinib
RAF1 (CRAF) dabrafenib
RET ponatinib, regorafenib, vandetanib, dasatinib, sorafenib
RET[G691S] * staurosporine
RET[G691S][non-activated] cabozantinib
RET[M918T] * staurosporine
RET[M918T][non-activated] staurosporine
RET[S891A] * staurosporine
RET[S891A][non-activated] quizartinib
RET[V804M] * staurosporine
RET[V804M][non-activated] staurosporine
RET[Y791F] * staurosporine
RET[Y791F][non-activated] cediranib
ROCK1 GSK-429286A
SPHK1 PF-543 citrate
SRC A-770041, ponatinib, regorafenib
SRPK1 staurosporine
SYK * staurosporine
SYK[non-activated] staurosporine
TBK1 staurosporine
TGFβR1(TGFBR1) SB 431542
TIE2(TEK) * ponatinib, vandetanib
TNIK bosutinib, sunitinib
TRKA(NTRK1) * AZ23, ponatinib
TRKA(NTRK1)[non-activated] AZ23, ponatinib
TRKB(NTRK2) * AZ23, ponatinib
TRKB(NTRK2)[non-activated] ponatinib
TRKC(NTRK3) * AZ23, sorafenib
TYRO3 * BMS-777607
TYRO3[non-activated] BMS-777607
WEE1 AZD1775
WNK1 WNK463
WNK4 WNK463
YES(YES1) staurosporine, saracatinib

* 精製後活性向上の為ATP処理を施しているキナーゼ蛋白質

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