CHR-3996 Inhibitor CAS No. 1235859-13-8

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Chemical Characteristic

Product Name	CHR-3996
CAS No.	1235859-13-8
Molecular Weight	393.41
Formula	C₂₁H₂₀FN₅O₂
Chemical Name	?2-[6-[(6-fluoroquinolin-2-yl)methylamino]-3-bicyclo[3.1.0]hexanyl]-N-hydroxypyrimidine-5-carboxamide
Smiles	c1(ncc(cn1)C(=O)NO)C1CC2C(C1)C2NCc1nc2c(cc1)cc(cc2)F
Chemical Structure

Biological activities

CHR-3996 is a class I selective orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM. The K_{i of CHR-3996 is 4.8 nM against HDAC. CHR-3996 shows excellent potency against the class I isoforms, HDAC1, HDAC2, and HDAC3, and good selectivity over HDAC5 and HDAC6 which are members of the class II family. CHR-3996 inhibits HDAC1, HDAC2, and HDAC3 with IC50 of 3, 4 and 7 nM, respectively. In contrast, CHR-3996 prevents HDAC5 and HDAC6 activities with an IC50 of 0.2 and 2.1 µM. CHR-3996 inhibits the proliferation of HCT116 with a GI50 of 72 nM. CHR-3996 exhibits growth inhibition of series of tumor cell proliferations in the range 31738764;750 nM. CHR-3996 inhibits LoVo cells (colon carcinoma), A2780 (ovarian adenocarcinoma) and Du145 (prostate adenocarcinoma) with GI50 of 140, 210 and 48 nM, respectively, while CHR-3996 blocks the proliferation of Molt-4 (acute lymphoblastic leukemia), Hut78 (T-cell lymphoma) and U937 (histiocytic lymphoma) with GI50 of 31, 31 and 52 nM, respectively. CHR-3996 (50 mg/kg po) is administered for 14 days to female nude BALB/c mice in 5% DMSO-saline bearing the HCT116 colon carcinoma xenograft. CHR-3996 substantially reduces tumor volume and demonstrates an apparent dose dependency. ^[1]}

Protocols

CHR-3996 (30 µM) is dissolved in 0.3% DMSO .^[1]

References

[1] Moffat D, Discovery of 2-(6-{[(6-fluoroquinolin-2-yl) methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor. J Med Chem. 2010, 53(24): 8663-8678.

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