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CAS No. : 1801765-04-7
MCE 国际站:Batoprotafib
产品活性:Batoprotafib (TNO155) 是一种有效的,选择性的,和具有口服活性野生型 SHP2 的变构抑制剂 (IC50= 0.011 μM)。Batoprotafib 有研究 RTK 依赖性恶性肿瘤的潜力,尤其是晚期实体瘤。
研究领域:Protein Tyrosine Kinase/RTK | Metabolic Enzyme/Protease
作用靶点:SHP2 | Phosphatase
In Vitro: Batoprotafib shows an IC50 of 0.008 μM in KYSE520 pERK assay and shows an IC50 of 0.100 μM in KYSE520 5-day cell proliferation assay. The off-target IC50 values are 18 μM, 6.9 μM, and 11 μM for Cav1.2, VMAT, and SST3, respectively. Batoprotafib (0-1000 nM; 6 days) inhibits the viability of NCI-H3255, HCC827, and PC9 cells with IC50 values lower than 1.5 μM. Batoprotafib is efficacious in EGFR-mutant NSCLC cell lines.
Batoprotafib is efficacious in acquired resistance models of EGFR inhibitors and demonstrates combination benefit with EGFR inhibitors.
Batoprotafib enhances the efficacy of KRASG12C inhibitors against KRASG12C lung and colorectal cancers.
Batoprotafib inhibits immune-suppressive macrophages and synergizes with PD1 blockade.
In Vivo: The oral bioavailability in mouse, rat and money are 78%, 86%, and 60%, respectively.
Batoprotafib (20 mg/kg; p.o.; twice daily for 40 days) inhibits tumor growth and is more effective when combined with Dabrafenib (HY-14660) plus Trametinib (HY-10999) in nude mice bearing HT-29 xenografts.
Batoprotafib (7.5 mg/kg; p.o.; b.i.d. or q.d. for 36 days) plus JDQ-443 (HY-139612) (100 mg/kg; p.o.; q.d.) improves the single-agent activity of JDQ443 in KRASG12C-mutated cell-derived (CDX) models in nude mice.
相关产品:Covalent Screening Library Plus | Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Metabolism/Protease Compound Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Covalent Screening Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Phosphatase Inhibitor Library | Anti-Prostate Cancer Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | BN82002 | Rubrofusarin 6-O-β-D-glucopyranoside | PF-04577806 | RMC-3943 | GNF362 | MY10 | D-erythro-Sphingosine | AS1949490 | NTPDase-IN-1 | SHP099 hydrochloride | Ertiprotafib | Trimyristin--d15 | SMAP-2 | cyt-PTPε Inhibitor-1 | Raphin1 acetate | Calyculin A | Endothall | Razuprotafib | Icerguastat | Methyl pseudolarate B | 5-FAM-Alkyne | Calcium glycerophosphate | Trichomide A | PTP1B-IN-21 | PFKFB3-IN-2 | CD31 | CCT007093 | BVT948 | L-690330 hydrate | SPI-112
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货号: HY-136173
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