| + |
ponatinib | down-regulates activity 
chemical inhibition
|
KIT |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259272 |
|
|
Homo sapiens |
HMC-1 Cell |
| pmid |
sentence |
| 23539538 |
Ponatinib was found to inhibit the kinase activity of KIT G560V and KIT D816V in the human mast cell leukemia cell line HMC-1. In addition, ponatinib was found to block Lyn- and STAT5 activity in neoplastic mast cells |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
FGFR2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259278 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23468082 |
Ponatinib is an oral multitargeted kinase inhibitor that potently inhibits all 4 members of the FGFR family. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
LYN |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259273 |
|
|
Homo sapiens |
Mast Cell |
| pmid |
sentence |
| 23539538 |
Ponatinib was found to inhibit the kinase activity of KIT G560V and KIT D816V in the human mast cell leukemia cell line HMC-1. In addition, ponatinib was found to block Lyn- and STAT5 activity in neoplastic mast cells |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates
chemical inhibition
|
ABL1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-206277 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
RIPK3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261083 |
|
|
Homo sapiens |
JURKAT Cell |
| pmid |
sentence |
| 25801024 |
Discovery of ponatinib as the first-in-class dual inhibitor of RIPK1 and RIPK3 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates
chemical inhibition
|
SRC |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-206280 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
FGFR3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259279 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23468082 |
Ponatinib is an oral multitargeted kinase inhibitor that potently inhibits all 4 members of the FGFR family. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
PDGFRA |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261985 |
|
|
in vitro |
|
| pmid |
sentence |
| 23430109 |
AP24534 also inhibited SRC (IC50: 5.4 nM) and members of the VEGFR, FGFR, and PDGFR families of receptor tyrosine kinases (Table 1 and Table S1) |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
STAT5A |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259274 |
|
|
Homo sapiens |
Mast Cell |
| pmid |
sentence |
| 23539538 |
Ponatinib was found to inhibit the kinase activity of KIT G560V and KIT D816V in the human mast cell leukemia cell line HMC-1. In addition, ponatinib was found to block Lyn- and STAT5 activity in neoplastic mast cells |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
RET |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259275 |
|
|
Homo sapiens |
Leukemia Cell, Medullary Thyroid Carcinoma Cell |
| pmid |
sentence |
| 23526464 |
The RET tyrosine kinase encoding gene acts as a dominantly transforming oncogene in thyroid carcinoma and other malignancies. Ponatinib (AP24534) is an oral ATP-competitive tyrosine kinase inhibitor that is in advanced clinical experimentation in leukemia.Ponatinib is a potent inhibitor of RET kinase and has promising preclinical activity in models of RET-driven medullary thyroid carcinoma. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
RIPK1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261082 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 25801024 |
Discovery of ponatinib as the first-in-class dual inhibitor of RIPK1 and RIPK3 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
FGFR4 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259280 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23468082 |
Ponatinib is an oral multitargeted kinase inhibitor that potently inhibits all 4 members of the FGFR family. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
BCR-ABL |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259268 |
|
|
Homo sapiens |
Myeloid Leukemia Cell |
| pmid |
sentence |
| 23409026 |
Pre-existing BCR-ABL mutations can be detected in a substantial number of chronic-phase CML patients by sensitive allele-specific PCR technique using CD34+ cells. These mutations are associated with imatinib resistance if affecting drug binding directly or indirectly. After the recent approval of nilotinib, dasatinib, bosutinib and ponatinib for treatment of chronic myeloid leukemia along with imatinib, all of which vary in their effectiveness against mutated BCR-ABL forms, detection of pre-existing BCR-ABL mutations can help in selection of appropriate first-line drug therapy. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259277 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23468082 |
Ponatinib is an oral multitargeted kinase inhibitor that potently inhibits all 4 members of the FGFR family. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259276 |
|
|
Homo sapiens |
Non-small Cell Lung Cancer Cell |
| pmid |
sentence |
| 23563700 |
Ponatinib was able to significantly inhibit the growth of primary lung cancer cultures in vitro. Our data indicate that pharmacological inhibition of FGFR1 kinase activity with ponatinib may be effective for the treatment of lung cancer patients whose tumors overexpress FGFR1. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
KDR |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261984 |
|
|
in vitro |
|
| pmid |
sentence |
| 23430109 |
AP24534 also inhibited SRC (IC50: 5.4 nM) and members of the VEGFR, FGFR, and PDGFR families of receptor tyrosine kinases (Table 1 and Table S1) |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
FLT3 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261983 |
|
|
in vitro |
|
| pmid |
sentence |
| 23430109 |
We assessed the in vitro activity of ponatinib against clinically relevant FLT3-ITD mutant isoforms that confer resistance to AC220 or sorafenib. Substitution of the FLT3 "gatekeeper" phenylalanine with leucine (F691L) conferred mild resistance to ponatinib, but substitutions at the FLT3 activation loop (AL) residue D835 conferred a high degree of resistance. |
|
| Publications: |
1 |
Organism: |
In Vitro |
3.0
ponatinib
