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ZM 306416 {[allProObj[0].p_purity_real_show]}

货号:A331607 同义名: CB 676475

ZM-306416 is an inhibitor of VEGFR (Flk-1 or KDR) and Flt with IC50 of 100 nM and 2 μM. It also shows inhibition activity against Src and Abl with IC50 values of 0.33μM and 1.3μM, respectively.

ZM 306416 化学结构 CAS号:690206-97-4
ZM 306416 化学结构
CAS号:690206-97-4
ZM 306416 3D分子结构
CAS号:690206-97-4
ZM 306416 化学结构 CAS号:690206-97-4
ZM 306416 3D分子结构 CAS号:690206-97-4
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ZM 306416 纯度/质量文件 产品仅供科研

货号:A331607 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 EGFR/ErbB1 ErbB3 ErbB4 HER2/ErbB2 mutant EGFR 其他靶点 纯度
WZ-3146 ++++

EGFR (E746_A750/T790M), IC50: 14 nM

EGFR (E746_A750), IC50: 2 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 (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

98%
Osimertinib ++

L858R/T790M EGFR, IC50: 11.44 nM

WT EGFR, IC50: 12.92 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/T790M), IC50: 8 nM

EGFR (L858R), IC50: 2 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 (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

98+%
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 Caspase,PARP 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

++++

EGFRT790M, IC50: 0.79 nM

EGFRL858R/T790M, IC50: 0.51 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 (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

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(C797S/T790M/del19), IC50: 67.2 nM

EGFR(del19), IC50: 39.9 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 ++++

EGFRd746-750/T790M/C797S, IC50: 0.26 nM

EGFRL858R/T790M, IC50: 0.19 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 ALK1 ALK2 ALK3 ALK4 ALK6 Smad3 TGF-β TGFβRI/ALK5 TGFβRII 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

++++

ALK2, IC50: 1.3 nM

+

ALK3, IC50: 85.8 nM

+

ALK4, IC50: 2133 nM

+

ALK5, IC50: 9276 nM

99%+
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

98%
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

99%+
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%
LDN-214117 ++

ALK2, IC50: 24 nM

98%
DMH-1 +

ALK2, IC50: 107.9 nM

99%+
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

99%+
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

99%+
Alantolactone 98%
SIS3 97%
Pirfenidone 98%
Hesperetin 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

98%
GW788388 +++

ALK5, IC50: 18 nM

98%
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

98%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

99%+
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

99%+
Galunisertib ++

TβRI, IC50: 56 nM

98%
SB 431542 +

ALK5, IC50: 94 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 Abl Bcr-Abl 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

99%+
KW-2449 +++

Abl (T315I), IC50: 4 nM

Abl, IC50: 14 nM

FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

RET 99%+
Rebastinib ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

FLT3,Tie-2 99%+
PP121 ++

Abl, IC50: 18 nM

VEGFR,PDGFR 99%+
GNF-7 +++

M351T, IC50: 133 nM

E255V, IC50: 122 nM

99%+
Olverembatinib dimesylate ++++

Abl, IC50: 0.34 nM

Abl (G250E), IC50: 0.35 nM

99%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

98+%
GNF-2 +

Bcr-Abl (K562 cell line), IC50: 273 nM

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

DUB 98+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

98%
Radotinib ++

BCR-ABL1, IC50: 34 nM

98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 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 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 98%
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

FGFR,c-Kit,PDGFR 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/KDR, IC50: 37 nM

VEGFR2/Flk1, IC50: 270 nM

+

VEGFR3/FLT4, IC50: 660 nM

c-Kit,c-Fms 99%+
Axitinib ++++

VEGFR1/FLT1, IC50: 0.1 nM

++++

VEGFR2/KDR, IC50: 0.2 nM

VEGFR2/Flk1, IC50: 0.18 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

+++

mVEGF2, IC50: 165 nM

hVEGFR2, IC50: 9 nM

+

hVEGFR3, IC50: 420 nM

98%
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

98%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

c-Kit 98+%
SU 5402 ++

VEGFR2, IC50: 20 nM

98%
Rivoceranib 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 98%
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 98%
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。

ZM 306416 生物活性

靶点
  • VEGFR1

    VEGFR1, IC50:0.33 μM

描述 ZM-306416, a vascular endothelial growth factor receptor (VEGFR) antagonist, was identified as a potent inhibitor of EGFR function[3]. The VEGFR1/2 inhibitors, ZM306416 and KRN633, lead to a dose-dependent decrease in mineralization[4]. ZM-306416 induced selective anti-proliferative effect toward the EGFR addicted NSCLC cell lines H3255 and HCC4011 (IC50=0.09±0.007 μM and 0.072±0.001 μM respectively), while sparing the wild type EGFR cell lines A549 and H2030 (IC50>10 μM). ZM-306416 is also found to inhibit the ABL in vitro kinase activity with a less potent IC50 value of 1.3±0.2 μM toward the ABL kinase[3]. Ki8751, a selective VEGFR2 inhibitor, completely suppressed the effect of VEGF121 on SCE cell permeability, although ZM306416, a selective VEGFR1 inhibitor, did not affect the VEGF121-induced decrease in TEER (transendothelial electrical resistance)[5].

ZM 306416 参考文献

[1]Antczak C, Mahida JP, et al. A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen. 2012 Aug;17(7):885-99.

[2]Wilkinson J, Hallis T, et al. Development and validation of a cell-based assay for the nuclear receptor retinoid-related orphan receptor gamma. Assay Drug Dev Technol. 2011 Apr;9(2):125-35.

[3]Antczak C, Mahida JP, Bhinder B, Calder PA, Djaballah H. A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen. 2012 Aug;17(7):885-99

[4]McLaughlin KI, Milne TJ, Zafar S, Zanicotti DG, Cullinan MP, Seymour GJ, Coates DE. The in vitro effect of VEGF receptor inhibition on primary alveolar osteoblast nodule formation. Aust Dent J. 2020 Sep;65(3):196-204

[5]Fujimoto T, Inoue T, Maki K, Inoue-Mochita M, Tanihara H. Vascular Endothelial Growth Factor-A Increases the Aqueous Humor Outflow Facility. PLoS One. 2016 Sep 1;11(9):e0161332

ZM 306416 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.00mL

0.60mL

0.30mL

14.98mL

3.00mL

1.50mL

29.96mL

5.99mL

3.00mL

ZM 306416 技术信息

CAS号690206-97-4
分子式C16H13ClFN3O2
分子量 333.745
别名 CB 676475
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 50 mg/mL(149.82 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
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