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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
200 Results for "
In vivo antitumor activity
" in MedChemExpress (MCE) Product Catalog:
Products (200)
200 Results for "In vivo antitumor activity" in MCE Product Catalog:
13
13 Publications Verification
Target:
Research Areas:
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo .
11
11 Cited Publications
Target:
Research Areas:
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
8
8 Cited Publications
Research Areas:
Adenosine dialdehyde, a purine nucleoside analogue, is a potent inhibitor of S-Adenosylhomocysteine hydrolase (SAHH) (Ki=3.3 nM) . Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research .
6
6 Cited Publications
CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo .
5
5 Cited Publications
Synonyms: SHR3162; Fuzuloparib
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
4
4 Cited Publications
Target:
Research Areas:
PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model .
4
4 Cited Publications
Cat. No.: HY-132192A
Purity: 99.26%
Target:
Research Areas:
PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model .
4
Target:
Checkpoint Kinase (Chk) VEGFR Src c-Fms Aurora Kinase FGFR FLT3 RET CDK
Research Areas:
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
4
Bimiralisib (PQR309) is an orally active, blood-brain barrier-penetrant PI3K/mTOR inhibitor with in vitro antiproliferative activity and in vivo antitumor activity. Bimiralisib induces G1 cell cycle arrest, apoptosis and cell death in cancer cells, while inhibiting cancer cell proliferation, migration, invasion, colony formation and spheroid generation. Bimiralisib upregulates the expression of E2F4. The combination of Bimiralisib with venetoclax enhances therapeutic efficacy in acute myeloid leukemia models. Bimiralisib can be used in cancer-related research .
3
3 Cited Publications
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability .
3
3
3 Cited Publications
Synonyms: BDTX-1535; EGFR-In-76
Target:
Research Areas:
Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
2
2 Cited Publications
Research Areas:
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo .
2
2 Cited Publications
Synonyms: L-2,4-DiamInobutyric acid
Category:
Neurological Disease Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Cancer
Target:
2
2 Cited Publications
Synonyms: L-2,4-DiamInobutyric acid hydrobromide
Category:
Neurological Disease Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Cancer
Target:
2
Elsulfavirine (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer .
1
1
1
1 Cited Publications
Cat. No.: HY-W039442
CAS No.: 64183-27-3
Target:
2′-Deoxy-2′-fluoroadenosine is a fluorinated deoxyadenosine with antitumor and antiviral activity, able to interfere with viral or cancer cell replication by being incorporated into DNA. 2′-Deoxy-2′-fluoroadenosine can be used for the synthesis of 2′-Deoxy-2′-fluoro-modified oligonucleotides hybridized with RNA. 2′-Deoxy-2′-fluoroadenosine can be cleaved efficiently by E. coli purine nucleoside phosphorylase (PNP) to the toxic agent 2-fluoroadenine (FAde). 2′-Deoxy-2′-fluoroadenosine shows excellent in vivo activity against tumors expressing E. coli PNP .
1
1 Cited Publications
PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
