货号:A114366 同义名: CZC-00008004;Dianilinopyrimidine-01
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
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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 |
++++
u-Abl1 (T315I), IC50: 5 nM p-Abl1 (native), IC50: 0.75 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 (G250E), IC50: 0.35 nM Abl, IC50: 0.34 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。 |
描述 | Aberrant tyrosine kinase activity plays a critical role in many hematologic disorders, including chronic myeloid leukemia characterized by the constitutive activity of BCR-ABL. ABL therefore represents a crucial target for new therapeutic strategies[3]. CZC-8004 is a pan-kinase inhibitor, with low micromolar IC50 values for tyrosine kinase including ABL kinase. A 50% bead loading gave the highest level of PK (protein kinase) identification for CZC-8004, extracting 55 PKs from a single cell lysate. The CZC-8004 beads extracted 61 and 64 PKs with 55 PKs common across the two bead batches examined[4]. |
[1]CZC-8004 is a pan-kinase inhibitor, with low micromolar IC50 values for tyrosine kinase.
[3]Cilloni D, Saglio G. Molecular pathways: BCR-ABL. Clin Cancer Res. 2012 Feb 15;18(4):930-7.
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.23mL 0.65mL 0.32mL |
16.16mL 3.23mL 1.62mL |
32.33mL 6.47mL 3.23mL |
CAS号 | 916603-07-1 |
分子式 | C17H16FN5 |
分子量 | 309.341 |
别名 | CZC-00008004;Dianilinopyrimidine-01 |
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,2-8°C |
溶解度 |
DMSO: 80 mg/mL(258.61 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 |