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Chemical Structure| 2244904-70-7 Chemical Structure| 2244904-70-7

Structure of BAY-293
CAS No.: 2244904-70-7

Chemical Structure| 2244904-70-7

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BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21nM.

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Product Citations

Product Citations

Wang, Cheng-xiang ; Wang, Ting-ting ; Zhang, Kun-dong ; Li, Ming-yu ; Shen, Qian-cheng ; Lu, Shao-yong , et al.

Abstract: Pancreatic ductal adenocarcinoma (PDAC) is currently one of the most lethal cancers worldwide. Several basic studies have confirmed that Kirsten rat sarcoma virus (KRAS) is a key driver gene for the occurrence of PDAC, and KRAS mutations have also been found in most patients in clinical studies. In this study, two pan-KRAS inhibitors, BI-2852 and BAY-293, were chosen as chemical probes to investigate their antitumor potency in PDAC. Their inhibitory effects on KRAS activation were validated in vitro and their antiproliferative potency in PDAC cell lines were profiled, with half-maximal inhibitory concentration (IC50) values of approximately 1 μM, demonstrating the therapeutic potential of pan-KRAS inhibitors in the treatment of PDAC. However, feedback regulation in the KRAS pathway weakened inhibitor activity, which was observed by a 50 times difference in BAY-293 from in vitro activity. Furthermore, pan-KRAS inhibitors effectively inhibited cell proliferation in 3D organoids cultured from PDAC patient samples; however, there were some variations between individuals. These results provide a sufficient theoretical foundation for KRAS as a clinical therapeutic target and for the application of pan-KRAS inhibitors in the treatment of PDAC, with important scientific significance in translational medicine.

Keywords: pancreatic ductal adenocarcinoma ; KRAS ; driver gene ; BAY-293 ; organoid

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Product Details of BAY-293

CAS No. :2244904-70-7
Formula : C25H28N4O2S
M.W : 448.58
SMILES Code : N(C1=NC(=NC2C=C(C(=CC=21)OC)OC)C)[C@@H](C1SC=C(C2C=CC=CC=2CNC)C=1)C
MDL No. :MFCD31813755
InChI Key :WEGLOYDTDILXDA-OAHLLOKOSA-N
Pubchem ID :137322663

Safety of BAY-293

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of BAY-293

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RD cells 0.2 µM BAY-293 significantly reduced MYC expression in RD cells. Sci Rep. 2025 Jan 23;15(1):2893.
BH837 3.7 µM 4 days Test the cytotoxicity of BAY-293 against NSCLC and PDAC cell lines Transl Oncol. 2021 Dec;14(12):101230.
BH828 1.7 µM 4 days Test the cytotoxicity of BAY-293 against NSCLC and PDAC cell lines Transl Oncol. 2021 Dec;14(12):101230.
BxPC3 5 µM 4 days Test the synergy of BAY-293 with 2-DG, showing synergistic effects. Discov Oncol. 2022 Sep 1;13(1):84.
AsPC1 5 µM 4 days Test the synergy of BAY-293 with 2-DG, showing synergistic effects. Discov Oncol. 2022 Sep 1;13(1):84.
TE671 cells 0.2 µM BAY-293 significantly reduced MYC expression in TE671 cells. Sci Rep. 2025 Jan 23;15(1):2893.
KCL-22-IMR cells 1.932 μM (alone), 1.732 μM (combined with imatinib) BAY-293 alone or in combination with imatinib showed similar inhibitory effects on the proliferation of KCL-22-IMR cells. Mol Ther Oncolytics. 2021 Nov 20;23:560-570.
KCL-22 cells 0.4, 0.8, 1.2, 1.6, 2.0 μM 48 hours BAY-293 inhibited the proliferation of KCL-22 and KCL-22-IMR cells in a dose-dependent manner. Mol Ther Oncolytics. 2021 Nov 20;23:560-570.
K1 cells 1 µM, 10 µM, 25 µM 24 hours To evaluate the effect of BAY-293 on thyroid cancer cell viability, results showed that BAY-293 significantly reduced cell viability in a concentration-dependent manner. Int J Mol Sci. 2025 Mar 13;26(6):2579.
FTC-133 cells 1 µM, 10 µM, 25 µM 24 hours To evaluate the effect of BAY-293 on thyroid cancer cell viability, results showed that BAY-293 significantly reduced cell viability in a concentration-dependent manner. Int J Mol Sci. 2025 Mar 13;26(6):2579.
8305C cells 1 µM, 10 µM, 25 µM 24 hours To evaluate the effect of BAY-293 on thyroid cancer cell viability, results showed that BAY-293 significantly reduced cell viability in a concentration-dependent manner. Int J Mol Sci. 2025 Mar 13;26(6):2579.
MIA PaCa-2 2.5 μM 24 hours BAY-293 promoted phosphorylation of ERK and AKT in a dose-dependent manner and increased expression of cleaved PARP, suggesting potential apoptosis promotion via feedback regulation. Acta Pharmacol Sin. 2022 Oct;43(10):2696-2708.
PANC-1 2.5 μM 72 hours BAY-293 inhibited ERK phosphorylation, and a rebound in protein expression and phosphorylation levels was observed at 48 h (pERK) and 72 h (pAKT). Acta Pharmacol Sin. 2022 Oct;43(10):2696-2708.
MIA PaCa-2 5 µM 4 days Test the synergy of BAY-293 with 2-DG, showing synergistic effects. Discov Oncol. 2022 Sep 1;13(1):84.
BH1522 cells 0.2 µM BAY-293 inhibited proliferation and suppressed MYC activity in BH1522 cells. Sci Rep. 2025 Jan 23;15(1):2893.
BH1406 NSCLC cells 1.12 µM 4 days BAY-293 significantly inhibited the viability of BH1406 cells with an IC50 value of 1.12 µM. Transl Lung Cancer Res. 2024 Nov 30;13(11):2987-2997.
BH1406 NSCLC cells 0.5 µM 72 hours BAY-293 treatment significantly reduced the expression levels of SOS1 and MYC. Transl Lung Cancer Res. 2024 Nov 30;13(11):2987-2997.
HT22 cells 2 μM 24 hours After inhibiting SOS1, the expression level of FBL was significantly reduced, indicating that BAY-293 regulates FBL expression by inhibiting SOS1, thereby reducing the inflammatory response. J Inflamm Res. 2024 Apr 11;17:2217-2231.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice BCR-ABL-independent imatinib resistance model Intraperitoneal injection 20 mg/kg Once daily for 7 days BAY-293 prolonged survival in a mouse model of BCR-ABL-independent resistance compared with saline or imatinib, showing significant efficacy. Mol Ther Oncolytics. 2021 Nov 20;23:560-570.
BALB/c nude mice ATC orthotopic model Intraperitoneal injection 10 mg/kg, 50 mg/kg 2 weeks To evaluate the antitumor effect of BAY-293 in an ATC orthotopic model, results showed that BAY-293 significantly improved pathological features and reduced tumor growth. Int J Mol Sci. 2025 Mar 13;26(6):2579.

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