Drug Class Detail

Drug Class SRC Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Apatinib Rivoceranib YN968D1 KIT Inhibitor 48 RET Inhibitor 36 SRC Inhibitor 26 VEGFR2 Inhibitor 34 Apatinib (YN968D1) is an inhibitor of receptor tyrosine kinases, including KDR (VEGFR2), RET, c-KIT, Src, and PDGFRa, which may result in reduced cell proliferation and inhibition of tumor growth (PMID: 21443688).
PP-121 ABL Inhibitor (pan) 8 mTOR Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 VEGFR2 Inhibitor 34 PP-121 inhibits several types of kinases including, PDGFR, Hck, mTOR, KDR (VEGFR2), Src and Abl to prevent cell proliferation (PMID: 24867098).
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).
Vandetanib Caprelsa ZD6474 ABL1 Inhibitor 4 EGFR Inhibitor (Pan) 38 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 30 Caprelsa (vandetanib) is a multi-tyrosine kinase inhibitor with activity against VEGFR, EGFR, RET, SRC, and ABL1 kinases, potentially resulting in decreased tumor growth (PMID: 25031937, PMID: 25490448). Caprelsa (vandetanib) is FDA approved for use in medullary thyroid cancer (FDA.gov).
KX2-391 KX-01 SRC Inhibitor 26 KX2-391 is a peptidomimetic dual inhibitor of Src and pretubulin, which results in tumor growth inhibition and metastasis prevention (PMID: 22784709).
Ponatinib Iclusig AP24534 BCR-ABL Inhibitor 23 DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR Inhibitor (Pan) 18 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-alpha Inhibitor 7 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 30 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).
CCT241161 RAF Inhibitor (Pan) 17 SRC Inhibitor 26 CCT241161 is a paradox-breaking pan-RAF inhibitor, with additional activity against SRC and LCK, which potentially results in decreased growth of tumors, including those resistant to BRAF inhibitors (PMID: 25500121).
NS-018 JAK2 Inhibitor - ATP competitive 14 SRC Inhibitor 26 YES Inhibitor 2 NS-018 inhibits JAK2, including JAK2 V617F, as well as SRC family members, including SRC, FYN, and YES, potentially leading to decreased cell proliferation (PMID: 24413068, PMID: 22829185).
AC-93253 iodide SRC Inhibitor 26 AC-93253 iodide is an inhibitor of SRC, which also results in reduced expression and phosphorylation of signaling molecules downstream of Src, potentially leading to decreased cell proliferation and inhibition of tumor growth (PMID: 29132432).
SKLB646 BRAF Inhibitor 18 CRAF Inhibitor 10 SRC Inhibitor 26 VEGFR2 Inhibitor 34 SKLB646 is a multi-kinase inhibitor with activity against Src, Kdr (Vegfr2), Braf and Craf, resulting in decreased downstream signaling and potentially leading to reduced tumor growth (PMID: 26721945).
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).
XL999 FGFR1 Inhibitor 21 FGFR3 Inhibitor 12 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 SRC Inhibitor 26 VEGFR2 Inhibitor 34 XL999 inhibits multiple tyrosine kinases including VEGFR2/KDR, FGFR1/3, PDGFR-beta, FLT3, RET, KIT, and SRC, which can result in anti-tumor activity (J Clin Oncol, 25:18s, 2007 (suppl;abstr 3591), PMID: 19581523).
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).
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).
Debio 0617B ABL Inhibitor (pan) 8 CSF1R Inhibitor 22 FLT3 Inhibitor 48 JAK Inhibitor (Pan) 8 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 30 Debio 0617B is a multi-kinase inhibitor of SRC, JAK, and ABL, the class III kinases, CSF1R, FLT3, KIT, and PDGFR, and the class V kinases, VEGFR 1/2/3, which may result in inhibition of Stat3 and Stat5 signaling, leading to inhibition of tumor cell growth and metastasis (PMID: 27439479).
CCT196969 RAF Inhibitor (Pan) 17 SRC Inhibitor 26 CCT196969 is a paradox-breaking pan-RAF inhibitor, with additional activity against SRC and LCK, which potentially results in decreased growth of tumor cells, including cells resistant to BRAF inhibitors (PMID: 25500121).
Si306 SRC Inhibitor 26 Si306 inhibits SRC, which may result in decreased tumor cell growth (PMID: 27196762).
Repotrectinib TPX-0005 ALK Inhibitor 19 JAK2 Inhibitor 17 ROS1 Inhibitor 14 SRC Inhibitor 26 Trk Receptor Inhibitor (Pan) 23 Repotrectinib (TPX-0005) is a multi-kinase inhibitor that demonstrates strong activity against Ros1, Ntrk1/2/3, and Alk, and also inhibits Jak2 and Src family kinases, resulting in tumor cell death (PMID: 30093503).
BPR1J373 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 30 BPR1J373 is a derivative of 5-phenylthiazol-2-ylamine-pyriminide that inhibits multiple tyrosine kinases including KIT, FLT3, VEGFR1, 2, 3, PDGFR-alpha, PDGFR-beta, RET, and SRC, and may result in anti-tumor activity (PMID: 27512117).
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).
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).
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).
UM-164 p38 MAPK Inhibitor (Pan) 2 SRC Inhibitor 26 UM-164 is a small molecule that binds to a specific inactive conformation of Src, resulting in inhibition of Src downstream signaling and inhibits p38 MAPKs, resulting in growth inhibition, and apoptosis in tumor cells (PMID: 27154914).
SU6656 SRC Inhibitor 26 SU6656 is a small molecule inhibitor of SRC, which may lead to inhibition of tumor growth and decreased tumor invasion and angiogenesis (PMID: 22244830).
Bosutinib Bosulif SKI-606 ABL Inhibitor (pan) 8 AXL Inhibitor 24 BTK inhibitor 20 SRC Inhibitor 26 TNK2 Inhibitor 6 Bosulif (bosutinib) inhibits SRC and ABL kinases, and has additional activity against other kinases including AXL, TNK2, BTK, resulting in decreased pathway activation and inhibition of tumor cell proliferation (PMID: 12543790, PMID: 19039322, PMID: 26555154). Bosulif (bosutinib) is FDA approved for use in patients with Ph+ (BCR-ABL) chronic myelogenous leukemia (FDA.gov).
Molecular Profile Protein Effect Treatment Approaches
CSF3R S783fs loss of function SRC Inhibitor
CSF3R Q741* loss of function - predicted SRC Inhibitor
CSF3R Y752* loss of function - predicted SRC Inhibitor
CSF3R inact mut loss of function SRC Inhibitor