Drug Class Detail

Drug Class BCR-ABL Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Saracatinib AZD0530 BCR-ABL Inhibitor 23 SRC Inhibitor 26 Saracatinib (AZD0530) is a multi-kinase inhibitor with activity against ABL and SRC, which may block proliferation, metastasis, and survival in cancer cells (PMID: 19393585).
PD173955 BCR-ABL Inhibitor 23 SRC Inhibitor 26 PD173955 is a tyrosine kinase inhibitor of Src and Bcr-Abl, which can result in anti-mitotic activity, induce apoptosis, and inhibit cell growth (PMID: 12154026, PMID: 10626805).
RXDX-105 AC013773|CEP-32496 ABL Inhibitor (pan) 8 ABL1 Inhibitor 4 BCR-ABL Inhibitor 23 BRAF Inhibitor 18 CRAF Inhibitor 10 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 VEGFR2 Inhibitor 34 RXDX-105 (CEP-32496) inhibits wild-type BRAF, BRAF V600E, c-RAF, ABL1 (and BCR-ABL), c-KIT, RET, PDGFR beta, and VEGFR2, potentially resulting in decreased tumor growth (PMID: 22319199).
AP23464 BCR-ABL Inhibitor 23 SRC Inhibitor 26 AP23464 is a dual kinase inhibitor of Src and Abl, which is capable of inducing apoptosis and cell cycle arrest as well as inhibiting cellular proliferation (PMID: 15256422, PMID: 16492148).
Radotinib IY5511 BCR-ABL Inhibitor 23 Radotinib inhibits BCR-ABL1, therefore results in growth inhibition of tumor cells (PMID: 25676420, PMID: 26065685).
PBA2 BCR-ABL Inhibitor 23 GSK-3beta Inhibitor 3 PBA2 is a dual BCR-ABL and GSK3-beta inhibitor that inhibits tumor cell growth (AACR, Cancer Res: April 2016; Volume 57, Abstract #3915).
Dasatinib Sprycel BMS-354825 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 BTK inhibitor 20 CSF1R Inhibitor 22 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 TNK2 Inhibitor 6 Sprycel (dasatinib) is an inhibitor of the SRC-family of protein kinases, BCR-ABL, and ABL, and has additional activity against other kinases including KIT, DDR1/2, PDGFRA/B, and EPHA2, which prevents cell growth (PMID: 25709401, PMID: 25284748, PMID: 18797457). Sprycel (dasatinib) is FDA approved for both Philadelphia chromosome positive adult and pediatric chronic myelogenous leukemia and adult acute lymphoblastic leukemia (FDA.gov).
ON044580 BCR-ABL Inhibitor 23 JAK2 Inhibitor 16 ON044580 is a non-ATP competitive inhibitor of BCR-ABL, BCR-ABL (T315I), JAK2, and JAK2(V617F), which may inhibit cell proliferation through inhibition of STAT5 signaling (PMID: 20717479).
Flumatinib HH-GV678 BCR-ABL Inhibitor 23 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Flumatinib inhibits KIT, PDGFR, and BCR-ABL, potentially resulting in decreased tumor cell proliferation (NCI Drug Dictionary).
Ponatinib Iclusig AP24534 BCR-ABL Inhibitor 23 DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR Inhibitor (Pan) 17 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 29 Iclusig (ponatinib) inhibits the Bcr-Abl fusion, and other tyrosine kinases, such as RET, DDR, VEGFR, FGFR, KIT, and FLT3 (PMID: 23526464, PMID: 25284748, PMID: 19878872). Iclusig (ponatinib) is FDA approved for chronic myeloid leukemia (CML) and Philadelphia chromosome positive acute lymphoblastic leukemia (Ph positive ALL) as well as ABL1 T315I CML and ABL1 T315I Ph positive ALL (FDA.gov).
PD166326 BCR-ABL Inhibitor 23 SRC Inhibitor 26 PD166326 is a dual kinase inhibitor of Src and Abl, which can inhibit cellular growth and induce apoptosis (PMID: 12684394, PMID: 15657179).
XL228 BCR-ABL Inhibitor 23 IGF-1R Inhibitor 17 SRC Inhibitor 26 XL228 inhibits multiple tyrosine kinases, including the insulin-like growth factor 1 receptor (IGF1R), Src tyrosine kinase, and Bcr-Abl tyrosine kinase, which can lead to cell growth inhibition (Mol Cancer Ther 2009;8(12 Suppl):C192).
Imatinib mesylate Gleevec CGP-57148B|STI571 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 CSF1R Inhibitor 22 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Gleevec (imatinib mesylate) is a multi-target inhibitor of c-Kit, Pdgfr, and Bcr-Abl (NCI Drug Dictionary). Gleevec (imatinib mesylate) is FDA approved for c-KIT positive GIST and dermatofibrosarcoma protuberans, Philadelphia chromosome positive chronic myeloid leukemia, and FIP1L1-PDGFRA positive chronic eosinophilic leukemia (FDA.gov).
AZD0424 BCR-ABL Inhibitor 23 SRC Inhibitor 26 AZD0424 is a tyrosine kinase inhibitor of Abl and Src kinases, which may result in apoptosis and tumor growth inhibition (PMID: 25662515, PMID: 17704648).
C086 BCR-ABL Inhibitor 23 HSP90 Inhibitor 35 C086 inhibits HSP90 and BCR-ABL, resulting in decreased proliferation of tumor cells, including imatinib-resistant cells (PMID: 25501124).
Asciminib ABL001 BCR-ABL Inhibitor 23 Asciminib (ABL001) is an allosteric inhibitor of BCR-ABL that binds to a unique location outside the ATP binding site, resulting in decreased BCR-ABL kinase activity and reduced tumor growth (Blood Dec 2014, 124 (21) 398).
Bafetinib NS-187|INNO-406 BCR-ABL Inhibitor 23 DDR1 Inhibitor 8 DDR2 inhibitor 7 Bafetinib (NS-187) is a tyrosine kinase inhibitor with activity against Lyn, SRC kinase, DDR1/2, and BCR-ABL, but not the T315I mutation (PMID: 21154127, PMID: 19890374).
Danusertib PHA-739358 ABL1 Inhibitor 4 AURK Inhibitor (Pan) 11 BCR-ABL Inhibitor 23 FGFR1 Inhibitor 21 RET Inhibitor 36 TrkA Receptor Inhibitor 7 Danusertib (PHA-739358) is a pan-Aurora kinase with additional activity against ABL, FGFR1, RET, TRKA, and BCR-ABL, including the T315I mutant (PMID: 20072840, PMID: 18089710).
Nilotinib Tasigna AMN-107 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 CSF1R Inhibitor 22 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 Tasigna (nilotinib) inhibits several tyrosine kinases including BCR-ABL, PDGFR, KIT, DDR and CSF-1R, potentially resulting in reduced tumor cell proliferation (PMID: 21419934, PMID: 25284748). Tasigna (nilotinib) is FDA approved for use in patients with Ph+ chronic myeloid leukemia (FDA.gov).
Tozasertib MK-0457|VX-680 AURK Inhibitor (Pan) 11 BCR-ABL Inhibitor 23 Tozasertib (VX-680) is a pan-AURK inhibitor with increased potency against Aurora kinase A (AURKA), and has additional activity against BCR-ABL, potentially resulting in decreased tumor growth (PMID: 14981513, PMID: 22772060).
K0706 BCR-ABL Inhibitor 23 K0706 is a Bcr-Abl kinase inhibitor with activity against the T315I mutation, which may demonstrate potential antineoplastic activity (PMID: 29866888).
PD180970 BCR-ABL Inhibitor 23 SRC Inhibitor 26 PD180970 is an ATP-competitive tyrosine kinase inhibitor of Src and Abl, which can result in the inhibition of autophosphorylation and induce apoptosis (PMID: 10974196, PMID: 12499247).
rebastinib DCC-2036 BCR-ABL Inhibitor 23 FLT3 Inhibitor 48 TIE2 Inhibitor 1 VEGFR2 Inhibitor 34 Rebastinib (DCC-2036) inhibits the Bcr-Abl fusion and to a lesser extent, the receptor tyrosine kinases TIE-2, FLT3, and VEGFR2 (PMID: 21481795).
Molecular Profile Protein Effect Treatment Approaches