EGFR-IN-88 (Compound 4i) is an EGFR inhibitor (IC50: 87 nM). EGFR-IN-88 shows cytotoxicity against A549 cell with an IC50? of 3.902? μM. EGFR-IN-88 can induce cell apoptosis[1].
GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. IC50 Value: 0.34/0.68 nM(Bce-Abl wt/T315I) [1]Target: Bcr-Abl in vitro: GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. It also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy.in vivo: GZD824 induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I) [1]. Clinical trial: GZD824 is on the way of unknown clinical status.
Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays.
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities[1].
Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
Paltimatrectinib (compound I-147) is a potent tyrosine kinase inhibitor with an IC50 of <10 nM for tropomyosin kinases A (TrkA). Paltimatrectinib has the potential for cancer and inflammatory diseases[1].
Benz-AP is a potent photosensitizer. Benz-AP produces singlet oxygen, with a negative correlation with hCES2 (Human carboxylesterase 2) activity. Benz-AP displays a higher photocytotoxicity potency in cancer cells under low hCES2 environments. Upon TPE (Two-photon excitation), Benz-AP produces ROS and kills cancer cells and tumor spheroids[1].
ABP 215 (Bevacizumab-awwb), a Bevacizumab (Bevacizumab (HY-P9906)) biosimilar, is a humanized IgG1 monoclonal antibody targeting VEGFA (VEGFR). ABP 215 has anticancer effects, and can be used metastatic colorectal cancer (mCRC) research[1][2].
Lck-IN-1 is a potent lymphocyte protein tyrosine kinase (Lck) inhibitor extracted from patent WO2007013673A1, example 48[1].
Syk-IN-8 (compound 19q) is a Syk inhibitor, with antiproliferative activity against multiple hematological tumour cells. Syk-IN-8 inhibits PLCγ2 phosphorylation, can be used for research in blood cancers[1].
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37 nM for binding affinity to ALK[1].
PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].
GZD856 is a novel PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities[1].
Lamalbid is a natural product that can be found in Lantana montevidensis. Lamalbid inhibits ROS generation[1].
RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research[1].
BTK IN-1 is a potent BTK inhibitor, with an IC50 of <100 nM.
CpCDPK1/TgCDPK1-IN-1 (compound 7p) is a potent CpCDPK1/TgCDPK1 dual inhibitor (IC50: 10 nM and 5.0 nM respectively). CpCDPK1/TgCDPK1-IN-1 also inhibits Abl and Src (IC50: 75 nM and 65 nM respectively). CpCDPK1/TgCDPK1-IN-1 can be used for research of toxoplasmosis[1].
JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively.
IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC50 of 160 nM.
Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.
ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect[1].
GW806742X is a Mixed Lineage Kinase Domain-Like (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and anti-necroptosis activity. GW806742X has activity against VEGFR2[1][2].
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the treatment of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
AZ1495 (compound 28) is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL)[1].
Immepip dihydrobromide is a H3 agonist. Immepip dihydrobromide can reduce cortical histamine release. Immepip dihydrobromide can be used for the research of neurological diseases[1].
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM.
BTK inhibitor 4b is a potent, highly selective inhibitors of BTK with IC50 of 4.2 and 0.9 nM against activated and unactivated BTK, respectively; demonstrates significant efficacy in models in vivo and good ADME and safety profiles.
Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an 50 of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects[1].
Radotinib(IY-5511) is a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.IC50 value: 34 nM [1]Target: BCR-ABL1 inhibitorRadotinib is a BCR-ABL1 specific 2nd-generation tyrosine kinase inhibitor. According to recently conducted in vitro kinase assays, the IC50 value for radotinib against wild-type BCR-ABL1 kinase was 34 nM, which is relatively lower compared with the IC50 levels of c-kit (1,324 nM), PDGFR (PDGFRα, 75.5 nM; PDGFRβ, 130 nM) and src (>2,000 nM). Also, radotinib effectively inhibited the proliferation of common mutant clones of BCR-ABL1, with the exception of T315I. In an off-target kinase assay to assess safety, DDR, EPHB, LYN, and PDGFR kinases were inhibited below the 180 nM level.
TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells[1].