Bcr-Abl
Catalog No. | Inhibitor Name | Bcr-Abl | Abl | Other |
---|---|---|---|---|
A10290 | Dasatinib | **** | **** | Src,c-Kit (D816V),c-Kit (wt) |
A10468 | Imatinib Mesylate | * | c-Kit,PDGFR | |
A10108 | Saracatinib | ** | c-Src,LCK,EGFR (L861Q) | |
A10080 | Ponatinib | **** | **** | PDGFRα,VEGFR2,FGFR1 |
A10644 | Nilotinib | ** | ||
A10715 | Danusertib | ** | ** | Aurora A,TrkA,RET |
A10095 | AT9283 | *** | JAK3,JAK2,Aurora B | |
A10988 | Degrasyn | * | DUB | |
A10119 | Bafetinib | *** | *** | Lyn |
A10508 | KW-2449 | ** | *** | FLT3 (D835Y),FLT3,FGFR1 |
A10661 | NVP-BHG712 | * | EphB4,C-Raf,c-Src | |
A11200 | Rebastinib | *** | FLT3,KDR,Tie-2 | |
A15849 | GZD824 Dimesylate | **** | **** | |
A11439 | GNF-2 | * | ||
A15887 | GNF-7 | *** | * | |
A13029 | Radotinib | ** | ||
A16320 | Dasatinib Monohydrate | **** | **** | Src,c-Kit (D816V),c-Kit (wt) |
A13237 | GNF-5 | * | ||
A13120 | PD173955 | *** | Src | |
A11379 | DPH | |||
A13530 | Flumatinib mesylate | **** | PDGFRβ, c-Kit |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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Flumatinib
Catalog No. A16258 multi-kinase 抑制剂Flumatinib是一种多激酶抑制剂,对c-Abl,PDGFRbeta和c-Kit的IC50值分别为1.2 nM,307.6 nM和2662 nM。 了解更多 -
Radotinib (IY-5511)
Catalog No. A13029 -
AST 487
Catalog No. A15003 -
WP1130 (Degrasyn)
Catalog No. A10988 DUB/Bcr/ABL 抑制剂WP1130 (Degrasyn)是一种新型的选择性小分子去泛素酶抑制剂和Bcr/Abl破坏途径激活剂,可特异性和快速下调野生型和突变型Bcr/Abl蛋白,而不会影响慢性粒细胞性白血病(CML)中的bcr/abl基因表达细胞。 了解更多 -
Nilotinib monohydrochloride monohydrate
Catalog No. A15186 -
NRC-AN-019
Catalog No. A13562 Bcr-Abl 抑制剂NRC-AN-019是Bcr-Abl蛋白-酪氨酸激酶的口服酪氨酸激酶抑制剂(TKI)。NRC-AN-019在抑制MDAMB231和HTB20/BT474细胞的血管生成潜力和增殖方面更有效。 了解更多 -
GZD824
Catalog No. A16264 -
PD173955
Catalog No. A13120 Bcr-Abl 抑制剂PD-173955是src酪氨酸激酶抑制剂。PD173955抑制Bcr-Abl依赖的细胞生长。PD173955显示G(1)中的细胞周期停滞。PD173955在Bcr-Abl的激酶抑制测定中的IC(50)为1-2 nM,在细胞生长测定中,其抑制Bcr-Abl依赖性底物酪氨酸磷酸化。 PD173955抑制试剂盒配体依赖性c-kit自磷酸化(IC(50)=约25 nM)和试剂盒配体依赖性M07e细胞增殖(IC(50)= 40 nM),但对白介素3依赖性(IC (50)= 250 nM)或粒细胞巨噬细胞集落刺激因子(IC(50)= 1 microM)依赖性细胞生长。 了解更多 -
GNF 2
Catalog No. A11439 -
Lyn-IN-1
Catalog No. A16265 -
SNIPER(ABL)-062
Catalog No. A18567 ABL inhibitorSNIPER(ABL)-062, in which an ABL inhibitor is linked to a ligand of cIAP1 via a linker containing a variable polyethylene glycol (PEG) unit, shows a potent activity to degrade the BCR-ABL protein. 了解更多 -
CHMFL-ABL-121
Catalog No. A19079 ABL2 inhibitorCHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively. 了解更多 -
CHMFL-ABL-039
Catalog No. A13182 BCR-ABL inhibitorCHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia. 了解更多 -
BCR-ABL-IN-1
Catalog No. A12496 BCR-ABL inhibitorBCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia. 了解更多 -
CHMFL-ABL/KIT-155
Catalog No. A12421 ABL/c-KIT dual kinase inhibitorCHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor. 了解更多 -
1-Naphthyl PP1 hydrochloride
Catalog No. A21790 Src/c-Abl inhibitor1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively). 了解更多 -
BCR-ABL-IN-2
Catalog No. A21043 inhibitor of BCR-ABL1 tyrosine kinaseBCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively. 了解更多 -
GZD824 Dimesylate
Catalog No. A15849 Bcr-Abl 抑制剂GZD824 Dimesylate是Bcr-Abl(WT)和Bcr-Abl(T315I)的新型生物可用Bcr-Abl抑制剂,IC50分别为0.34 nM和0.68 nM。 了解更多 -
Flumatinib mesylate
Catalog No. A13530 c-Abl/c-Kit/PDGRFβ 抑制剂Flumatinib mesylate以时间和剂量依赖性的方式降低U266细胞中C-MYC,HIF-1a和VEGF的表达,因此甲磺酸氟马替尼可能成为MM治疗的新药。 了解更多 -
Nilotinib (AMN-107)
Catalog No. A10644 Bcr-Abl 抑制剂Nilotinib (AMN-107)是一种Bcr-Abl抑制剂,IC50小于30 nM。 了解更多 -
DCC-2036 (Rebastinib)
Catalog No. A11200 Bcr-Abl 抑制剂DCC-2036 (Rebastinib)是一种Bcr-Abl抑制剂,作用于Abl1(WT)和Abl1(T315I),IC50分别为0.8 nM和4 nM,也抑制SRC, LYN, FGR, HCK, KDR, FLT3,和Tie-2,对c-Kit具有低的抑制活性。 了解更多 -
NVP-BHG712
Catalog No. A10661 EphB4 抑制剂NVP-BHG712是EphB4激酶的选择性抑制剂,在体外对EphB4的选择性超过40多种其他激酶(包括FGFR3)。 了解更多 -
Imatinib Mesylate
Catalog No. A10468 Bcr-Abl 抑制剂Imatinib mesylate是一种选择性酪氨酸激酶抑制剂,通过抑制KIT信号转导途径,在治疗胃肠间质瘤中诱导了持续的客观反应。 了解更多 -
Dasatinib (BMS-354825)
Catalog No. A10290 Abl-Src 抑制剂Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL,Src,c-Kit,ephrin受体和其他几种酪氨酸激酶,但不是erbB激酶,例如EGFR或Her2。 了解更多 -
Bafetinib (INNO-406)
Catalog No. A10119 Bcr-Abl 抑制剂Bafetinib (INNO-406)是一种双重Bcr-Abl/Lyn酪氨酸激酶抑制剂。 了解更多 -
Danusertib (PHA-739358)
Catalog No. A10715 Aurora 抑制剂Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂,在无细胞分析中的IC50为13 nM/79nM/61 nM,对Abl,TrkA,c-RET和FGFR1以及更低的浓度具有中等效力 对Lck,VEGFR2/3,c-Kit,CDK2等有效。 了解更多 -
AP24534 (Ponatinib)
Catalog No. A10080 BCR-ABL 抑制剂AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。 了解更多 -
Saracatinib (AZD0530)
Catalog No. A10108 Src/Abl 抑制剂Saracatinib (AZD0530)是一种高选择性,双特异性Src/Abl激酶抑制剂,对c-Src和Abl激酶的IC50分别为2.7和30 nM。 了解更多 -
Imatinib (Gleevec)
Catalog No. A10259 PDGFR 抑制剂Imatinib (Gleevec)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。 了解更多