INK128, Free Base (MLN-0128, Sapanisertib, CAS 1224844-38-5), >99%
LC Laboratories' Product Number I-3344 - INK128, Free Base (MLN-0128, Sapanisertib, CAS 1224844-38-5), >99% - for research use only. INK128 is a potent mTOR kinase inhibitor with a Ki of 1.4 nM. It had therapeutic benefit for prostate cancer metastasis. INK128 potently blocked cell proliferation in various breast cancer cell lines harboring PIK3CA (IC50 = 1.5-53 nM), PTEN (IC50 = 1-149 nM), KRAS and/or BRAF mutations (IC50 = 13-162 nM), and in human endothelial cells (IC50 = 33-40 nM) in vitro. In vivo, INK128 suppressed primary tumor growth significantly in both non-VEGF and VEGF-driven MCF-7 xenograft models. INK128 inhibited proliferation of B-cell acute lymphoblastic leukemia (B-ALL) cell lines in vitro and suppressed colony formation by primary human leukemia cells from adult and pediatric B-ALL patients. INK128 enhanced the efficacy of dasatinib in Philadelphia Chromosome-positive (Ph+) specimens. In a syngeneic mouse model of lymphoid BCR-ABL+ disease, INK128 rapidly cleared leukemic outgrowth. In non-Ph+, B-ALL xenografts, INK128 had a cytostatic effect. The addition of lapatinib to INK-128 treatment resulted in inhibition of both PI3K/Akt/mTOR and ERK pathways and prevented both HER2 and HER3 phosphorylation induced by INK-128. This dual blockade demonstrated antitumor activity in preclinical models of breast cancer resistant to anti-HER2 therapy.
Supplier | LC Laboratories |
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Product # | I-3344 |
Sku # | I-3344_50mg |
Pricing | 50 mg, $236.00 |
Citations for this product:
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bioRxiv - Cancer Biology 2021Quote: ... TAK228 (I-3344, LC Laboratories), and BYL-719 (CT-BYL719 ...
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Evolutionarily divergent mTOR remodels the translatome to drive rapid wound closure and regenerationbioRxiv - Developmental Biology 2021Quote: ... 100 mM (or 30.933 mg/mL) INK128 (LC Laboratories, I-3344) stock was prepared and stored at -80°C ...