mia paca-2

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

BN82002 (CDC25 Phosphatase Inhibitor I) is a synthetic inhibitor of CDC25 phophatases

Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. It diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into cells in vivo, exhibiting potent proapoptotic, antiproliferative, and differentiation-inducing effects.

3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.

Bleomycin Sulfate (Blenoxane) is a glycopeptide antibiotic, an inhibitor of DNA synthesis. Bleomycin Sulfate causes DNA strand breaks but not RNA strand breaks. Bleomycin Sulfate has antitumor activity.

LL-37, Human acetate is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity.

Royleanone possesses cytotoxic activity against the human pancreatic cancer cell line MIA PaCa-2.

Sodium Oxamate (Oxamic acid sodium salt) is an LDH inhibitor that specifically inhibits LDHA. Sodium Oxamate has antitumor activity and induces cell cycle arrest and apoptosis.

Gemcitabine hydrochloride (LY 188011 hydrochloride) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

C75 is an inhibitor synthetic fatty-acid synthase (FASN) and inhibits prostate cancer cells PC3 (IC50: 35 μM).C75 increases CPT1 activity and reduces DIO.

LXH254 is a B C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.

Chromomycin A3 is an antibiotic produced by Streptomyces sp that binds to gc-rich DNA sequences in the presence of divalent cations and inhibits DNA replication and transcription; it is also used as a fluorescent DNA stain and assay; and it has anticancer activity against diseases such as Hodgkin's, lung adenocarcinomas, melanomas, and breast cancer.

Oxythiamine (Hydroxythiamin) is an antivitamin of thiamine and a transketolase (TK) inhibitor. Oxythiamine inhibits cancer cell proliferation and induces cell cycle arrest. Oxythiamine has potential anticancer activity, inhibits non-oxidative synthesis of ribose, and induces apoptosis.

HedgehogIN-7 (Compound 8g), a purine derivative, acts as an inhibitor of the Hedgehog signaling pathway by reducing the expression of Hedgehog genes and inhibiting signal transmission. This compound exhibits significant cytotoxicity and selectivity towards Mia-PaCa-2 pancreatic cancer cells that are dependent on the Hedgehog pathway, making it useful for research in pancreatic cancer.

MEK RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K Akt mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.

KRAS G12D inhibitor 25 (Compound 148) acts as an inhibitor for KRAS G12C and HSP90α, displaying IC50 values of <0.1 μM and 0.1-1 μM respectively. Additionally, it suppresses the proliferation of MIA PaCa-2 and NCI-H358 cell lines, with EC50 values of <0.1 μM and 0.1-1 μM correspondingly. This compound also promotes the degradation of ERBB2, exhibiting a DC50 of 0.1-1 μM.

SOS1-IN-17 (Compound 8d) is an orally active inhibitor targeting the SOS1-KRASG12C interaction, with an IC50 of 5.1 nM. It suppresses ERK phosphorylation in DLD-1 cells with an IC50 of 18 nM and demonstrates antiproliferative activity in KRASG12C-mutant Mia-Paca-2 cells, with an IC50 of 0.11 μM. In mouse models, SOS1-IN-17 shows antitumor efficacy against pancreatic cancer.

KRAS G12C inhibitor 69 (Compound K09) is an inhibitor of the mutant RAS protein KRAS G12C with an IC50 of 4.36 nM. In the cell lines NCI-H358 and MIA-PACA-2, it suppresses ERK phosphorylation with IC50 values of 12 nM and 7 nM, respectively. Additionally, KRAS G12C inhibitor 69 hinders the proliferation of NCI-H358 and MIA-PACA-2 cancer cells, with IC50 values of 3.15 nM and 2.33 nM, respectively.

Anticanceragent 264 (Compound 5w) is an anticancer compound that exhibits significant antiproliferative activity in tumor cell lines, with an IC50 range of 7.5-33.67 μM. It notably induces cell cycle arrest at the G2 M phase in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines. This compound reduces key cell cycle proteins CDK1, CDK2, and Cyclin B1 in a dose-dependent manner and has strong binding activity with differentiation inhibitors and DNA-binding proteins. Anticanceragent 264 is useful for research in the cancer disease domain.

Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.

KRASG12C IN-15 (Compound 21) is an orally active KRASG12C inhibitor that effectively blocks SOS1-mediated GDP GTP exchange with an IC50 of 19 nM. It inhibits ERK phosphorylation with an IC50 of 0.051 μM and reduces the viability of KRASG12C mutant MIA PaCa-2 cells with an IC50 of 0.023 μM. Additionally, KRASG12C IN-15 demonstrates antitumor activity in a MIA PaCa-2 xenograft mouse model.