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Diazepinomicin (TLN 4601, ECO-4601) is a brain penetrant inhibitor of Ras-RAF-MAPK pathway post Ras prenylation and prior to MEK activation, binds the central and/or peripheral benzodiazepine receptors (PBR, TSPO); prevents EGF-induced phosphorylation of Raf-1, MEK, and ERK1/2; reduces Ras-GTP levels and induces apoptosis; shows antitumor activity and decreases tumor Raf-1 protein levels in MIA PaCa-2 tumor-bearing mice.

Brain Cancer

Phase 2 Discontinued




AZD1390 (AZD-1390) is a novel potent, selective, orally available and CNS penetrant ATM inhibitor with IC50 of 0.78 nM, displays >1,000-fold selectivity over closely related (PIKKs) and distant kinases; radiosensitises a panel of glioblastoma multiforme (GBM) cell lines and NCI-H2228 lung cells (IC50=3 nM); demonstrates potential in combination with radiation therapy for the treatment of brain tumors.

Brain Cancer

Phase 1 Clinical




CYC065 is a derivative of seliciclib and second generation CDK inhibitor that is mainly active on CDK2/5/9; demonstrates cytotoxicity both in MM cell lines sensitive as well as resistant to conventional chemotherapy with IC50 of 0.06-2 uM; blocks cells in the G1 phase and inhibits cell growth specifically in CCNE1-overexpressing USCs; significantly reduces tumour growth in xenografts derived from CCNE1-amplified USCs, shows synergistic effect in vitro and in vivo combined with Taselisib .

Brain Cancer

Phase 1 Clinical




CBL0137 (Curaxin CBL0137) is a histone chaperone FACT (facilitates chromatin transcription) and MYC signal inhibitor that markedly reduced tumor initiation and progression in vivo; simultaneously activates p53 and inhibits NF-κB without causing detectable genotoxicity, causes phosphorylation of p53 Ser(392) by CK2 and inhibition of NF-κB-dependent transcription in neuroblastoma cells; eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.

Brain Cancer

Phase 1 Clinical




IDH 305 (IDH305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C; exhibits >200 fold selectivity over WT IDH1 (IC50=6.14 uM), and no activtiy against IDH2 mutants; inhibits EGF-independent proliferation of HCT116-IDH1R132H+/- cells with IC50 of 20 nM; exhibits in vivo correlation of 2-HG reduction and efficacy in IDH1 mutant xenograft tumor model.

Brain Cancer

Phase 1 Clinical




LB-100 (LB100) is a potent serine/threonine protein phosphatase 2A (PP2A) inhibitor; exhibits inhibitory effect in HCC cell lines Huh-7, HepG2, Hep3B, and SNU-449 with mean IC50 of 10 uM; synergistically enhances the activity of doxorubicin and induces expression of HIF-1α and VEGF; significantly enhances tumor growth inhibition by cisplatin in vivo.

Brain Cancer

Phase 1 Clinical



1224844-38-5 Sapanisertib (INK-128, MLN0128) is a potent, ATP-competitive, orally active dual mTORC1/2 inhibitor with Ki of 1.4 nM in cell-free assays, >200-fold selectivity over calss I PI3K isoforms; inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2; also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors; shows tumor growth inhibition efficacy in multiplexenograft models.

Brain Cancer

Phase 2 Clinical

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