CUDC-101是一种强效的HDAC、EGFR和HER2抑制剂,IC50值分别为4.4、2.4和15.7 nM。它是一种包含炔基的砌块化学探针,用于铜催化的偶联反应(CuAAc)。
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产品名称 | HD1 ↓ ↑ | HD2 ↓ ↑ | HDAC ↓ ↑ | HDAC1 ↓ ↑ | HDAC10 ↓ ↑ | HDAC11 ↓ ↑ | HDAC2 ↓ ↑ | HDAC3 ↓ ↑ | HDAC4 ↓ ↑ | HDAC5 ↓ ↑ | HDAC6 ↓ ↑ | HDAC7 ↓ ↑ | HDAC8 ↓ ↑ | HDAC9 ↓ ↑ | 其他靶点 | 纯度 | |||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Givinostat HCl monohydrate |
++++
HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM |
+++
HD2, IC50: 10 nM |
99%+ | ||||||||||||||||
MC1568 |
++
HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM |
96% | |||||||||||||||||
Trichostatin A |
++++
HDAC, IC50: ~1.8 nM |
99%+ | |||||||||||||||||
Scriptaid | ✔ | 99%+ | |||||||||||||||||
Valproic acid sodium | ✔ | Autophagy | 97% | ||||||||||||||||
AR-42 |
+++
HDAC, IC50: 30 nM |
99%+ | |||||||||||||||||
Dacinostat |
+++
HDAC, IC50: 32 nM |
98+% | |||||||||||||||||
CUDC-101 |
++++
HDAC, IC50: 4.4 nM |
++++
HDAC1, IC50: 4.5 nM |
+++
HDAC10, IC50: 26.1 nM |
+++
HDAC2, IC50: 12.6 nM |
++++
HDAC3, IC50: 9.1 nM |
+++
HDAC4, IC50: 13.2 nM |
+++
HDAC5, IC50: 11.4 nM |
++++
HDAC6, IC50: 5.1 nM |
+
HDAC7, IC50: 373 nM |
++
HDAC8, IC50: 79.8 nM |
++
HDAC9, IC50: 67.2 nM |
HER2,EGFR | 99%+ | ||||||
M344 |
++
HDAC, IC50: 100 nM |
99%+ | |||||||||||||||||
Splitomicin |
+
Sir2p, IC50: 60 μM |
95% | |||||||||||||||||
Panobinostat |
++++
HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM |
98% | |||||||||||||||||
Sodium 4-Phenylbutyrate | ✔ | 98% | |||||||||||||||||
Vorinostat |
+++
HDAC, IC50: ~10 nM |
98% | |||||||||||||||||
Curcumin | ✔ | NF-κB,Nrf2 | 98% | ||||||||||||||||
Belinostat |
+++
HDAC, IC50: 27 nM |
98% | |||||||||||||||||
RG-2833 |
++
HDAC1, Ki: 32 nM |
++
HDAC3, Ki: 5 nM |
98% | ||||||||||||||||
Valproic acid |
+
HDAC1, IC50: 0.4 mM |
98% | |||||||||||||||||
BG45 |
+
HDAC1, IC50: 2 μM |
+
HDAC2, IC50: 2.2 μM |
+
HDAC3, IC50: 289 nM |
99%+ | |||||||||||||||
Entinostat |
+
HDAC1, IC50: 0.51 μM |
+
HDAC3, IC50: 1.7 μM |
98% | ||||||||||||||||
Resminostat |
+++
HDAC1, IC50: 42.5 nM |
++
HDAC3, IC50: 50.1 nM |
++
HDAC6, IC50: 71.8 nM |
98+% | |||||||||||||||
Romidepsin |
+++
HDAC1, IC50: 36 nM |
+++
HDAC2, IC50: 47 nM |
99%+ | ||||||||||||||||
Parthenolide | ✔ | NF-κB,p53 | 97% HPLC | ||||||||||||||||
Tacedinaline |
+
HDAC1, IC50: 0.9 μM |
+
HDAC2, IC50: 0.9 μM |
+
HDAC3, IC50: 1.2 μM |
98% | |||||||||||||||
Mocetinostat |
++
HDAC1, IC50: 0.15 μM |
+
HDAC11, IC50: 0.59 μM |
+
HDAC2, IC50: 0.29 μM |
+
HDAC3, IC50: 1.66 μM |
98% | ||||||||||||||
WT-161 |
++++
HDAC1, IC50: 8.35 nM |
+++
HDAC2, IC50: 15.4 nM |
++++
HDAC6, IC50: 0.4 nM |
99%+ | |||||||||||||||
Fimepinostat |
++++
HDAC1, IC50: 1.7 nM |
++++
HDAC10, IC50: 2.8 nM |
++++
HDAC11, IC50: 5.4 nM |
++++
HDAC2, IC50: 5.0 nM |
++++
HDAC3, IC50: 1.8 nM |
+++
HDAC6, IC50: 27 nM |
99%+ | ||||||||||||
Tucidinostat |
++
HDAC1, IC50: 95 nM |
++
HDAC10, IC50: 78 nM |
++
HDAC2, IC50: 160 nM |
++
HDAC3, IC50: 67 nM |
99%+ | ||||||||||||||
Santacruzamate A |
++++
HDAC2, IC50: 119 pM |
99%+ | |||||||||||||||||
(E,E)-RGFP966 |
++
HDAC3, IC50: 80 nM |
99%+ | |||||||||||||||||
LMK-235 |
+++
HDAC4, IC50: 11.9 nM |
++++
HDAC5, IC50: 4.2 nM |
99%+ | ||||||||||||||||
Tasquinimod | ✔ | 99%+ | |||||||||||||||||
CAY10603 |
++++
HDAC6, IC50: 2 pM |
98% | |||||||||||||||||
Tubastatin A |
+++
HDAC6, IC50: 15 nM |
98% | |||||||||||||||||
Tubacin |
++++
HDAC6, IC50: 4 nM |
99%+ | |||||||||||||||||
ACY-738 |
++++
HDAC6, IC50: 1.7 nM |
99%+ | |||||||||||||||||
Nexturastat A |
++++
HDAC6, IC50: 5 nM |
99%+ | |||||||||||||||||
BRD73954 |
+++
HDAC6, IC50: 36 nM |
++
HDAC8, IC50: 120 nM |
98% | ||||||||||||||||
Tubastatin A HCl |
+++
HDAC6, IC50: 15 nM |
+
HDAC8, IC50: 854 nM |
98% | ||||||||||||||||
PCI-34051 |
+++
HDAC8, IC50: 10 nM |
99%+ | |||||||||||||||||
Ricolinostat |
++
HDAC1, IC50: 58 nM |
++
HDAC2, IC50: 48 nM |
++
HDAC3, IC50: 51 nM |
++++
HDAC6, IC50: 4.7 nM |
++
HDAC8, IC50: 100 nM |
99%+ | |||||||||||||
Droxinostat |
+
HDAC3, IC50: 16.9 μM |
+
HDAC6, IC50: 2.47 μM |
+
HDAC8, IC50: 1.46 μM |
99%+ | |||||||||||||||
Abexinostat |
++++
HDAC1, Ki: 7 nM |
+++
HDAC10, IC50: 24 nM |
+++
HDAC2, Ki: 19 nM |
++++
HDAC3/SMRT, Ki: 8.2 nM |
+++
HDAC6, Ki: 17 nM |
+
HDAC8, IC50: 280 nM |
98%+ | ||||||||||||
Citarinostat |
+++
HDAC1, IC50: 35 nM |
+++
HDAC2, IC50: 45 nM |
+++
HDAC3, IC50: 46 nM |
++++
HDAC6, IC50: 2.6 nM |
++
HDAC8, IC50: 137 nM |
99%+ | |||||||||||||
HPOB |
+
HDAC1, IC50: 2.9 μM |
+
HDAC10, IC50: 3.0 μM |
+
HDAC2, IC50: 4.4 μM |
+
HDAC3, IC50: 1.7 μM |
++
HDAC6, IC50: 56 nM |
+
HDAC8, IC50: 2.8 μM |
97% | ||||||||||||
Quisinostat 2HCl |
++++
HDAC1, IC50: 0.11 nM |
++++
HDAC10, IC50: 0.46 nM |
++++
HDAC11, IC50: 0.37 nM |
++++
HDAC2, IC50: 0.33 nM |
++++
HDAC3, IC50: 4.86 nM |
++++
HDAC4, IC50: 0.64 nM |
++++
HDAC5, IC50: 3.69 nM |
++++
HDAC8, IC50: 4.26 nM |
99+% | ||||||||||
Domatinostat |
+
HDAC1, IC50: 1.20 μM |
+
HDAC10, IC50: 21 μM |
+
HDAC11, IC50: 9.7 μM |
+
HDAC2, IC50: 1.12 μM |
+
HDAC3, IC50: 0.57 μM |
+
HDAC5, IC50: 11.3 μM |
+
HDAC9, IC50: 50 μM |
99%+ | |||||||||||
TMP269 |
++
HDAC4, IC50: 157 nM |
++
HDAC5, IC50: 97 nM |
+++
HDAC7, IC50: 43 nM |
+++
HDAC9, IC50: 23 nM |
99%+ | ||||||||||||||
Pracinostat |
++
HDAC1, IC50: 49 nM |
+++
HDAC10, IC50: 40 nM |
++
HDAC11, IC50: 93 nM |
++
HDAC2, IC50: 96 nM |
+++
HDAC3, IC50: 43 nM |
++
HDAC4, IC50: 56 nM |
+++
HDAC5, IC50: 47 nM |
+
HDAC6, IC50: 1.008 μM |
++
HDAC7, IC50: 137 nM |
++
HDAC8, IC50: 140 nM |
++
HDAC9, IC50: 70 nM |
99%+ | |||||||
TMP195 |
++
HDAC4, Ki: 59 nM |
++
HDAC5, Ki: 60 nM |
+++
HDAC7, Ki: 26 nM |
+++
HDAC9, Ki: 15 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 | 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 |
98% | |||||||||||||||||
CNX-2006 |
++
mutant EGFR, IC50: <20 nM |
++
mutant EGFR, IC50: <20 nM |
98% | ||||||||||||||||
AZD3759 |
++++
EGFR (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM |
98% | |||||||||||||||||
Erlotinib |
++++
EGFR, IC50: 2 nM |
95% | |||||||||||||||||
Saracatinib |
+++
EGFR, IC50: 5 nM EGFR (L861Q), IC50: 4 nM |
99%+ | |||||||||||||||||
AG1557 | ✔ | 98% | |||||||||||||||||
Rociletinib |
++
EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM |
98% | |||||||||||||||||
AG490 |
+
EGFR, IC50: 0.1 μM |
98% | |||||||||||||||||
Cetuximab |
++++
EGFR, Kd: 0.39 nM |
98% | |||||||||||||||||
Osimertinib |
++
WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM |
99% | |||||||||||||||||
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 |
98+% | |||||||||||||||||
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 |
98% | |||||||||||||||||
Falnidamol | ✔ | 99%+ | |||||||||||||||||
AZ-5104 |
++++
EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 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 |
98+% | ||||||||||||||||
Lazertinib |
++++
WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 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 | 97% | ||||||||||||||||
Zipalertinib |
+++
EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 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 | ✔ | 99% | |||||||||||||||||
(S)-Sunvozertinib | ✔ | 98% | |||||||||||||||||
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 | ✔ | 98% | |||||||||||||||||
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 |
98+% | |||||||||||||||||
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 | 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 |
99+% | |||||||||||||||
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 |
Src,Raf | 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 (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM |
++
HER2, IC50: 14 nM |
98% | ||||||||||||||||
Canertinib dihydrochloride |
+++
EGFR, IC50: 7.4 nM |
+++
ErbB2, IC50: 9 nM |
98% | ||||||||||||||||
Allitinib tosylate |
++++
EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 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 |
98% | ||||||||||||||||
Afatinib |
++++
EGFR (L858R), IC50: 10 nM EGFR (wt), IC50: 0.5 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 |
98% | |||||||||||||||
Tuxobertinib |
++++
EGFR, Kd: 0.2 nM |
++++
HER2, Kd: 0.76 nM |
98% | ||||||||||||||||
ALK-IN-1 |
++
EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM |
ALK | 98+% | ||||||||||||||||
Brigatinib |
+
EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 nM |
FLT3,ALK | 98% | ||||||||||||||||
Avitinib |
++++
EGFR L858R/T790M, IC50: 0.18 nM |
BTK | 99%+ | ||||||||||||||||
EAI045 | ✔ | 97% | |||||||||||||||||
Almonertinib | ✔ | 98% | |||||||||||||||||
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 |
98% | |||||||||||||||||
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 | ✔ | 98% | |||||||||||||||||
Canertinib |
+++
ErbB2, IC50: 9.0 nM |
EGFR | 99%+ | ||||||||||||||||
(E/Z)-CP-724714 |
++
HER2/ErbB2, IC50: 10 nM |
98+% | |||||||||||||||||
Lapatinib |
+++
ErbB2, IC50: 9.2 nM |
EGFR | 98% | ||||||||||||||||
AEE788 |
++++
HER2/ErbB2, IC50: 6 nM |
EGFR | 98+% | ||||||||||||||||
Neratinib |
+
HER2, IC50: 59 nM |
EGFR,Src | 98% | ||||||||||||||||
BMS-599626 |
+
HER2, IC50: 30 nM |
99+% | |||||||||||||||||
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 | ✔ | 98% | |||||||||||||||||
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 | CUDC-101 is a potent, multi-acting inhibitor against histone deacetylases (HDAC), epidermal growth factor receptor (EGFR), and human epidermal growth factor receptor 2 (HER2) with IC50 values of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 had weak inhibition on the following proteins: KDR (VEGFR2) (849 nM), Src (11000 nM), Lyn (840 nM), Lck (5910 nM), Abl-1 (2890 nM), FGFR-2 (3430 nM), Flt-3 (1500 nM), and Ret (3200 nM). CUDC-101 exhibited strong anti-proliferative activity in many human cancer cell lines with IC50 value ranging from 0.04 – 0.80 μM[3]. The exposure of CUDC-101 (0.1, 1, or 10 μmol/L) for 5 to 24 hours increased acetylation of histone H3 and H4 in various cancer cell lines at a dose-dependent manner. CUDC-101 at 1 μmol/L also inhibited EGFR and HER2 phosphorylation and the level of antiapoptotic proteins, survivin, and Bcl-xL. By treating HCT-116 colon cancer cells with CUDC-101 (0.1, 1, or 10 μmol/L) for 24 hours, the activities of caspases 3 and 7 were significantly increased. In Hep-G2 liver cancer xenograft model, daily administration of 120 mg/kg CUDC-101 for 9 days significantly induced 30% tumor regression. Similarly, CUDC-101 (120 mg/kg/day) treatment showed significant inhibitory effect on tumor growth in A549 NSCLC cell- and MDA-MB-468 breast cancer cell-implanted mice[4]. |
作用机制 | CUDC-101 is a synthesized, multi-targeted inhibitor for HDAC, EGFR, and HER2. The structure of quinazoline is a well-characterized scaffold for the inhibition of EGFR and HER2. By incorporating a hydroxamic acid into the quinazoline pharmacophore with a proper spacer, this compound binds to HDAC to disrupt its enzyme activity[3]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human BxPC3 cells | Proliferation assay | Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay, IC50=0.27 μM | 20143778 | ||
human Capan1 cells | Proliferation assay | Antiproliferative activity against human Capan1 cells after hrs by ATP content assay, IC50=0.8 μM | 20143778 | ||
human H460 cells | Proliferation assay | Antiproliferative activity against human H460 cells after hrs by ATP content assay, IC50=0.7 μM | 20143778 | ||
human HCC827 cells | Proliferation assay | Antiproliferative activity against human HCC827 cells after hrs by ATP content assay, IC50=0.6 μM | 20143778 | ||
Dose | Mice: 80 mg/kg[3] (i.p.), 120 mg/kg[4] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.51mL 2.30mL 1.15mL |
23.02mL 4.60mL 2.30mL |
CAS号 | 1012054-59-9 |
分子式 | C24H26N4O4 |
分子量 | 434.488 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 25 mg/mL(57.54 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 |
动物实验配方 |