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CUDC-907
Cat No.
CEI-0869
Description
CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. Phase 1.
CAS No.
1339928-25-4
Molecular Weight
508.55
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
PI3Kɑ, HDAC1, HDAC2, HDAC3, HDAC10
IC50
19 nM; 1.7 nM; 5 nM; 1.8 nM; 2.8 nM
Molecular Formula
C23H24N8O4S
Chemical Name
N-hydroxy-2-(((2-(6-methoxypyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxamide
Solubility
DMSO 102 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
In vitro
CUDC-907 inhibits other PI3K isoforms such as PI3Kβ, PI3Kγ, PI3Kδ, PI3KɑH1047R and PI3KɑE545K with IC50 of 54 nM, 311 nM, 39 nM, 73 nM and 62 nM, respectively. Moreover, CUDC-907 also prevents HDAC subtypes HDAC8, HDAC6 and HDAC11 with IC50 of 191 nM, 27 nM and 5.4 nM, respectively. In addition, CUDC-907 suppresses other types of HDAC enzymatic activity with lower potency. CUDC-907 inhibits the growth of a series of B cell lymphoma such as Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi and Raji with IC50 of 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM and 9 nM, respectively. CUDC-907 also blocks the proliferation of Myeloma including RPMI8226, OPM-2 and ARH77 with IC50 of 2 nM, 1 nM and 5 nM, respectively. CUDC-907 displays greater anti-tumor activity in multiple myeloma and B cell lymphoma.
In vivo
CUDC-907 has a long half-life in murine tumors. CUDC-907 induces apoptosis and inhibits cancer cell proliferation in xenograft tumors. In efficacy studies in NHL and MM models, CUDC-907 is more efficacious than either a single-agent PI3K or HDAC inhibitor reference compound or a combination of the two agents given at maximally tolerated doses (MTD). Furthermore, CUDC-907 is more efficacious than the PI3Kδ-selective inhibitor CAL-101 when dosed at MTD doses.
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