货号:A144993 同义名: RXDX-105;CEP-32496
CEP-32496 is an inhibitor of BRAF V600E (IC50 = 14 nM), WT (IC50 = 34 nM) and c-Raf (IC50 = 39 nM). It also exhibits certain inhibitory activity against Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2.
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产品名称 | A-raf ↓ ↑ | B-Raf ↓ ↑ | C-Raf/Raf-1 ↓ ↑ | Raf ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Encorafenib | ✔ | 99%+ | |||||||||||||||||
GDC-0879 |
++++
B-Raf, IC50: 0.13 nM |
99%+ | |||||||||||||||||
SB-590885 |
++++
B-Raf, Ki: 0.16 nM |
99%+ | |||||||||||||||||
RAF265 | 99%+ | ||||||||||||||||||
Dabrafenib |
++++
B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM |
+++
C-Raf, IC50: 6.3 nM |
98% | ||||||||||||||||
Lifirafenib |
++++
WT A-RAF, IC50: 1 nM |
++
BRAF WT, IC50: 32 nM BRAF(V600E), IC50: 23 nM |
+++
C-RAF (Y340/341D), IC50: 7 nM |
EGFR | 98% | ||||||||||||||
ZM 336372 |
+
C-Raf, IC50: 70 nM |
99%+ | |||||||||||||||||
NVP-BHG 712 |
+
C-Raf, IC50: 0.395 μM |
99%+ | |||||||||||||||||
CCT196969 |
+
BRAF, IC50: 0.1 μM |
++
CRAF, IC50: 0.01 μM |
Src | 98% | |||||||||||||||
Vemurafenib |
++
B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM |
+
C-Raf, IC50: 48 nM |
98+% | ||||||||||||||||
PLX4720 |
++
B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM |
+++
C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM |
BRK | 99+% | |||||||||||||||
GW 5074 |
+++
C-Raf, IC50: 9 nM |
99%+ | |||||||||||||||||
Avutometinib |
+++
BRAF, IC50: 19 nM BRAF V600E, IC50: 8.2 nM |
+
CRAF, IC50: 56 nM |
98% | ||||||||||||||||
LY3009120 |
++++
BRAF WT, IC50: 15 nM BRAF(V600E), IC50: 5.8 nM |
++++
C-Raf, IC50: 4.3 nM |
99%+ | ||||||||||||||||
Agerafenib |
++
B-Raf, Kd: 36 nM B-Raf (V600E), Kd: 14 nM |
+
C-Raf, Kd: 39 nM |
RET | 99%+ | |||||||||||||||
TAK-632 |
+++
B-Raf, IC50: 8.3 nM |
++++
C-Raf, IC50: 1.4 nM |
99%+ | ||||||||||||||||
AZ 628 |
+
B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM |
++
C-Raf-1, IC50: 29 nM |
99% | ||||||||||||||||
PLX7904 | ✔ | 98+% | |||||||||||||||||
Sorafenib |
++
B-Raf (V599E), IC50: 38 nM B-Raf, IC50: 22 nM |
++++
Raf-1, IC50: 6 nM |
++++
Raf-1, IC50: 6 nM |
99% | |||||||||||||||
Tovorafenib | ✔ | 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 | 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, IC50: 14 nM Abl (T315I), IC50: 4 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 |
++++
p-Abl1 (native), IC50: 0.75 nM u-Abl1 (T315I), IC50: 5 nM |
Tie-2,FLT3 | 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 | c-RET ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Regorafenib |
+++
RET, IC50: 1.5 nM |
98% | |||||||||||||||||
TG101209 |
++
RET, IC50: 17 nM |
FLT3 | 99%+ | ||||||||||||||||
Danusertib |
+
RET, IC50: 31 nM |
99%+ | |||||||||||||||||
AD80 |
++++
RET V804M, IC50: 0.6 nM RET wt, IC50: 1.3 nM |
Raf,Src | 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 | 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 |
FLT3,c-Kit | 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/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM |
+
VEGFR3/FLT4, IC50: 660 nM |
c-Fms,c-Kit | 99%+ | ||||||||||||||
Axitinib |
++++
VEGFR1/FLT1, IC50: 0.1 nM |
++++
VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM |
98% | ||||||||||||||||
Dovitinib |
+++
VEGFR1/FLT1, IC50: 10 nM |
+++
VEGFR2/Flk1, IC50: 13 nM |
+++
VEGFR3/FLT4, IC50: 8 nM |
FLT3,c-Kit | 99%+ | ||||||||||||||
ZM 306416 |
+
VEGFR1, IC50: 0.33 μM |
Src | 99%+ | ||||||||||||||||
KRN-633 |
+
VEGFR1, IC50: 170 nM |
+
VEGFR2, IC50: 160 nM |
+
VEGFR3, IC50: 125 nM |
BTK,c-Kit | 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 |
FLT3,RET | 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。 |
产品名称 | c-Kit ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tyrphostin AG1296 |
+
c-Kit (Swiss 3T3), IC50: 1.8 μM |
PDGFR | 99%+ | ||||||||||||||||
Masitinib |
+
Kit, IC50: 200 nM |
99%+ | |||||||||||||||||
Motesanib Diphosphate |
+++
Kit, IC50: 8 nM |
98% | |||||||||||||||||
Ki8751 |
++
c-Kit, IC50: 40 nM |
98+% | |||||||||||||||||
Tivozanib |
++
c-Kit, IC50: 78 nM |
99%+ | |||||||||||||||||
Pazopanib |
+
c-Kit, IC50: 140 nM |
99% | |||||||||||||||||
Sitravatinib |
+++
Kit, IC50: 6 nM |
99%+ | |||||||||||||||||
Pexidartinib |
+++
Kit, IC50: 10 nM |
99%+ | |||||||||||||||||
Lactate |
++++
c-Kit, IC50: 2 nM |
FLT3 | 85% | ||||||||||||||||
Amuvatinib |
+++
c-Kit (D816H), IC50: 10 nM |
99%+ | |||||||||||||||||
Imatinib Mesylate |
+
c-Kit, IC50: 100 nM |
PDGFR | 99% | ||||||||||||||||
AZD2932 |
+++
c-Kit, IC50: 9 nM |
98% | |||||||||||||||||
Axitinib |
++++
Kit, IC50: 1.7 nM |
98% | |||||||||||||||||
Dovitinib |
++++
c-Kit, IC50: 2 nM |
FLT3 | 99%+ | ||||||||||||||||
Sunitinib | ✔ | FLT3 | 98% | ||||||||||||||||
OSI-930 |
+
Kit, IC50: 80 nM |
99%+ | |||||||||||||||||
Telatinib |
++++
c-Kit, IC50: 1 nM |
99%+ | |||||||||||||||||
Dasatinib monohydrate |
++
c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM |
Src | 98% | ||||||||||||||||
Dasatinib |
++
c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM |
Src | 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 | PDGFR ↓ ↑ | PDGFRα ↓ ↑ | PDGFRβ ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tyrphostin A9 |
+
PDGFR, IC50: 0.5 μM |
EGFR | 98% | ||||||||||||||||
Tyrphostin AG1296 | 99%+ | ||||||||||||||||||
Motesanib Diphosphate |
++
PDGFR, IC50: 84 nM |
98% | |||||||||||||||||
Pazopanib |
++
PDGFR, IC50: 84 nM |
99% | |||||||||||||||||
Imatinib |
+
PDGFR, IC50: 100 nM |
c-Kit | 98% | ||||||||||||||||
Imatinib Mesylate |
+
PDGFR, IC50: 100 nM |
c-Kit | 99% | ||||||||||||||||
Sennoside B | ✔ | 99%+ | |||||||||||||||||
PP121 |
++++
PDGFR, IC50: 2 nM |
VEGFR,mTOR | 99%+ | ||||||||||||||||
Crenolanib |
++++
PDGFRα, Kd: 2.1 nM |
++++
PDGFRβ, Kd: 3.2 nM |
99%+ | ||||||||||||||||
Masitinib |
+
PDGFRα, IC50: 540 nM |
+
PDGFRβ, IC50: 800 nM |
99%+ | ||||||||||||||||
Ki8751 |
++
PDGFRα, IC50: 67 nM |
c-Kit | 98+% | ||||||||||||||||
Tivozanib |
++
PDGFRα, IC50: 40 nM |
++
PDGFRβ, IC50: 49 nM |
99%+ | ||||||||||||||||
Ponatinib |
++++
PDGFRα, IC50: 1.1 nM |
98% | |||||||||||||||||
Amuvatinib |
++
PDGFRα (V561D), IC50: 40 nM |
99%+ | |||||||||||||||||
Axitinib |
+++
PDGFRα, IC50: 5.0 nM |
++++
PDGFRβ, IC50: 1.6 nM |
98% | ||||||||||||||||
CP-673451 |
+++
PDGFRα, IC50: 10 nM |
++++
PDGFRβ, IC50: 1 nM |
99%+ | ||||||||||||||||
Telatinib |
+++
PDGFRα, IC50: 15 nM |
c-Kit | 99%+ | ||||||||||||||||
Nintedanib |
++
PDGFRα, IC50: 59 nM |
++
PDGFRβ, IC50: 65 nM |
99+% | ||||||||||||||||
Avapritinib |
++++
PDGFRα (D842V), IC50: 0.5 nM |
99%+ | |||||||||||||||||
MK-2461 |
+++
PDGFRβ, IC50: 22 nM |
98%+ | |||||||||||||||||
Lactate |
+++
PDGFRβ, IC50: 27 nM |
FLT3,c-Kit | 85% | ||||||||||||||||
Linifanib |
++
PDGFRβ, IC50: 66 nM |
99%+ | |||||||||||||||||
AZD2932 |
+++
PDGFRβ, IC50: 4 nM |
c-Kit | 98% | ||||||||||||||||
Dovitinib |
+++
PDGFRβ, IC50: 27 nM |
FLT3,c-Kit | 99%+ | ||||||||||||||||
Sorafenib |
++
mPDGFRβ, IC50: 57 nM PDGFRβ, IC50: 57 nM |
99% | |||||||||||||||||
Sunitinib |
++++
PDGFRβ , IC50: 2 nM |
FLT3 | 98% | ||||||||||||||||
Orantinib |
+++
PDGFRβ, Ki: 8 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。 |
靶点 |
|
描述 | The Ras/RAF/MEK/ERK mitogen-activated protein kinase (MAPK) signaling pathway plays a central role in the regulation of cell growth, differentiation, and survival. The RAF members of this pathway consist of the serine/threonine kinases ARAF, BRAF, and CRAF, which phosphorylate and activate downstream MEK1/2. Expression of mutant BRAFV600E results in constitutive activation of the MAPK pathway, which can lead to uncontrolled cellular growth. CEP-32496 is a highly potent and orally efficacious inhibitor of BRAFV600E. It exhibits potent binding (BRAFV600E Kd = 14 nM) and cellular activity (pMEK IC50 = 82 nM and A375 proliferation IC50 = 78 nM). Administration of CEP-32496 to beagle dogs (single dose of 1 mg/kg iv and 10 mg/kg po) resulted in low clearance (CL = 5.0 (mL/min)/kg) and excellent bioavailability (%F = 100). CEP-32496 also exhibited a favorable CYP450 inhibition profile, with measured IC50 values greater than 10 μM versus the CYP1A2, 2C9, 2D6, and 3A4 isoforms and an IC50 = 3.4 μM versus 2C19. Athymic nude mice bearing established Colo-205 tumor xenografts were dosed orally with CEP-32496 at 10, 30, and100 mg/kg twice daily (BID) over a 14-day period. All doses were well tolerated without mortality or significant body weight loss. The 30 mg/kg dose group exhibited tumor stasis and a 40% incidence of partial tumor regressions (PRs) (p < 0.008), whereas the 100 mg/kg BID dose group exhibited both tumor stasis and an 80% incidence of PRs (p < 0.0001). Oral administration of CEP-32496 to Colo-205 tumor xenograft-bearing mice resulted in significant inhibition of pMEK in tumor cell lysates. For instance, a single 30 mg/kg (po) dose of CEP-32496 led to a 50 and 75% inhibition of normalized pMEK in tumor lysates at the 2 and 6 h postdose time point, respectively (p< 0.03)[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.93mL 0.39mL 0.19mL |
9.66mL 1.93mL 0.97mL |
19.33mL 3.87mL 1.93mL |
CAS号 | 1188910-76-0 |
分子式 | C24H22F3N5O5 |
分子量 | 517.457 |
别名 | RXDX-105;CEP-32496 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(96.63 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 |
15% Captisol+water 15 mg/mL suspension |