Cat. No. Name Size Price Add Cart
KI0518CUDC-9075 mg$432
CUDC-90710 mg$592
CUDC-90750 mg$1712
CUDC-907200 mg$3952

Chemical Characteristic

Product NameCUDC-907
CAS No.1339928-25-4
Molecular Weight 508.55
FormulaC23H24N8O4S
Chemical NameN-Hydroxy-2-[[[2-(6-methoxypyridin-3-yl)-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl](methyl)amino]pyrimidine-5-carboxamide
Smilesc1(ncc(cn1)C(=O)NO)N(C)Cc1cc2nc(nc(c2s1)N1CCOCC1)c1cnc(cc1)OC
Chemical Structure

Biological activities

CUDC-907 is a potent inhibitor of both HDAC and PI3K. CUDC-907 inhibits class I PI3K kinases (PI3Kα, PI3Kβ and PI3Kδ) with IC50 of 19, 54 and 39 nM, respectively. CUDC-907 durably inhibits the PI3K-AKT-mTOR pathway and compensatory signaling molecules such as RAF, MEK, MAPK, and STAT-3, as well as upstream receptor tyrosine kinases. CUDC-907 shows greater growth inhibition and proapoptotic activity than single-target PI3K or HDAC inhibitors in both cultured and implanted cancer cells.[1] CUDC-907 inhibits PI3Kα H1047R and PI3Kα E554655K with IC50 of 73 and 62 nM, respectively. CUDC-907 also inhibits HDAC subtypes (HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11) with IC50 of 1.7, 5.0, 1.8, 27, 2.8 and 5.4 nM, respectively. CUDC-907 potently inhibits proliferation of hematological cancer cell lines (B cell lymphoma, Myeloma). CUDC-907 is able to enhance antitumor activity when combined with standard of care agents in multiple myeloma and B cell lymphoma xenograft models. [2]

Protocols

For in vivo studies, CUDC-907 is formulated in 30% Captisol. [1]

References

[1] Qian C, et al. Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling. Clin Cancer Res. 2012, 18(15): 4104-4113.
[2] Bao R, et al. Antitumor Activity of CUDC-907, a dual PI3K and HDAC inhibitor in hematological cancer models. AACR Poster. 2012 # 3744.

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