# AACR ANNUAL MEETING 2023

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April 14-19, 2023

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Orange County Convention Center, 9800 International Dr, Orlando, FL 32819, US

## Insilico Medicine Presents Four Posters featuring AI-Designed Anti-Cancer Drugs at AACR

Insilico will present four novel inhibitors for the treatment of cancer developed with its end-to-end Pharma.AI platform. Drawing from trillions of data points and millions of compounds and molecular fragments, the platform uses generative AI for target identification and generative chemistry to produce new molecules.

- **Sujata Rao, MD**  
  Chief Medical Officer

- **Michelle Chen, PhD**  
  Chief Business Officer

Contact [bd@insilicomedicine.com](mailto:mailto:bd@insilicomedicine.com) for partnering opportunities

### Assets of Interest
- MAT2A
- USP1
- PHD
- KAT6A
- DGKA
- CDK12
- ENPP1
- cMYC

### Platform(s) of Interest
- PandaOmics
- Chemistry42
- inClinico

## MEET US AT AACR

### April 16-18

### Presentations:

**April 16**  
**13:30-17:00**  
[ISM3091, a novel selective USP1 inhibitor as a targeted anticancer therapy](https://www.abstractsonline.com/pp8/#!/10828/presentation/6560)  
**Poster #502**  
**Category:** Experimental and molecular therapeutics  
**Title:** Novel antitumor agents 2  
ISM3091 is an orally available and selective small molecule inhibitor of USP1, and demonstrated potential when targeted against a broad range of tumor lineages with HRD backgrounds. In vitro data showed potent anti-proliferation activity of the compound in BRCA-mutant tumor cells with excellent selectivity.

**April 16**  
**13:30-17:00**  
[ISM3412, a novel and selective MAT2A inhibitor for the treatment of cancer](https://www.abstractsonline.com/pp8/#!/10828/presentation/6562)  
**Poster #503**  
**Category:** Experimental and molecular therapeutics  
**Title:** Novel antitumor agents 2  
MAT2A is defined as a synthetic lethality target in MTAP-deleted cancers and plays an essential role in producing S-adenosylmethionine (SAM), a molecule involved in cell function and survival. As a potent and selective MAT2A inhibitor, ISM3412 demonstrated excellent drug-likeness with good solubility and permeability, good activity at low doses in animal models, and a favorable safety profile in preclinical studies.

**April 17**  
**9:00-12:30**  
[Targeting DGKA for immuno-oncology therapy: ISM4312A, a novel DGKA inhibitor with robust anti-tumor activity](https://www.abstractsonline.com/pp8/#!/10828/presentation/3559)  
**Poster #1855**  
**Category:** Immunology  
**Title:** Immunomodulatory agents and interventions 2  
Research indicates that DGKA mediates T-cell dysfunction during anti-PD-1 therapy, playing a role in the development of resistance to PD-1 blockade. ISM4312A is a novel DGKA inhibitor with excellent potency and high selectivity in cancer immunotherapy. The compound enhanced T-cell activity _in vitro_ and showed robust anti-tumor activities with or without anti-PD-1 therapy _in vivo_. Those data support the further evaluation of ISM4312A as a potential first-in-class DGKA inhibitor both as a single agent and in combination with a checkpoint inhibitor.

**April 18**  
**13:30-17:00**  
[Discovery and evaluation of ISM6466A, a novel covalent CDK12 inhibitor for the treatment of cancer](https://www.abstractsonline.com/pp8/#!/10828/presentation/8606)  
**Poster #4989**  
**Category:** Experimental and molecular therapeutics  
**Title:** Targeting protein kinases and phosphatases for therapy 1  
CDK12 inhibitors work synergistically with chemotherapy and PARP inhibitors and can be effective in a number of cancer types, including triple negative breast cancer, colorectal cancer, ovarian cancer, and hepatocellular carcinoma. Insilico's novel inhibitor, designed by its Pharma.AI platform, capitalizes on this cancer treatment approach that relies on the induction of the "BRCAness" phenotype.