T8634

8-Bromotheophylline (Bromotheophylline) is the active moiety of pamabrom, a mixture of 2-amino-2-methyl-propanol and bromotheophylline. From this mixture, 8-Bromotheophylline acts as a weak diuretic that has been used along with some analgesics to relieve the symptoms of premenstrual syndrome

CFT8634 is an orally active and selective degrader targeting BRD9, with effects on the proliferation of SMARCB1-deficient cancer cell lines. CFT8634 induces the formation of a ternary complex with BRD9 and E3 ligase, inducing BRD9 ubiquitination and subsequent degradation by the proteasome.

(S,R)-CFT8634 is a selective and orally active BRD9 protein degrader with potential for researching BRD9-mediated disorders, such as abnormal cellular proliferation [1].

EGFR mutant-IN-2 (Compound D51) is an inhibitor of EGFR mutants, specifically targeting EGFR L858R/T790M/C797S and EGFR del19/T790M/C797S mutants with IC50 values of 14 nM and 62 nM, respectively. This compound exhibits favorable pharmacokinetic (PK) parameters, safety properties, in vivo stability, and demonstrates antitumor activity [1].

EGFR T790M/L858R-IN-4, a potent inhibitor of EGFR T790M/L858R with anticancer properties (WO2024064091A1; Example 14) [1].

EGFR T790M/L858R-IN-5 (example 52) functions as a potent EGFR T790M/L858R inhibitor, demonstrating a 92.9% inhibition rate at a concentration of 0.05 μM [1].

EGFR T790M/L858R-IN-6 (compound 53), classified as a pyrimidine compound, serves as an effective inhibitor of EGFR T790M/L858R, demonstrating 90.88% inhibition of enzyme activity at a concentration of 0.05 μM [1].

EGFR T790M/L858R-IN-7 (Compound 72), a novel pyrimidine compound, exhibits high efficacy in inhibiting the EGFR T790M and L858R mutations, with a 93% inhibition rate at 0.05 μM. It achieves its inhibitory action by specifically binding to the kinase domain of EGFR, which prevents phosphorylation activity [1].

EGFR/c-Met-IN-2 (Compound H-22) is a dual inhibitor of EGFR/c-Met that arrests the G2/M phase to inhibit cell proliferation and demonstrates antitumor activity [1].