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M4693-15A MS-275 (Entinostat, SNDX-275, HDAC1/HDAC3 inhibitor) CAS: 209783-80-2

Specifications
References
CAS Number
209783-80-2
Grade
Highly Purified
Molecular Formula
C21H20N4O3
Molecular Weight
376.41
EU Commodity Code
38220090
UN DOT Shipping
UN2811 PGIII
Shipping Temp
Blue Ice
Storage Temp
-20°C
Carbamic acid, ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)-, 3-|pyridinylmethyl ester; Histone Deacetylase Inhibitor; SNDX-275; HDAC1/HDAC3 inhibitor

MS-275 is a synthetic benzamide derivative that inhibited partially purified human histone deacetylase (HDA) with an IC50 of 2uM and induced hyperacetylation of nuclear histones in tumor cell lines. MS-275 inhibited the proliferation of various human tumor cell lines such as A2780, Calu-3, HL-60, and K562 (IC50 values were 0.0415uM, 0.195uM, 0.212uM, and 0.589uM, respectively). MS-275 also inhibited the growth of human tumor xenografts in nude mouse.

Synonyms
Carbamic acid, ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)-, 3- pyridinylmethyl ester; Histone Deacetylase Inhibitor; SNDX-275; HDAC1/HDAC3 inhibitor
CAS No
209783-80-2
Molecular Weight
376.41
Molecular Formula
C21H20N4O3
Purity
≥99%
Appearance
Off-white powder
Melting Point
157-158.5ºC
Solubility
Soluble in DMSO at 25mg/ml with slight warming; very poorly soluble in ethanol and water; maximum solubility in plain water is estimated to be about 10-20uM. buffers, serum, or other additives may increase or decrease the aqueous solubility.
Calculated
C=67.01% H=5.36% N=14.88%
Storage and Stability
May be stored at RT for short-term only. Long-term storage is recommended at -20°C. Stable for 12 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards
 All products should be handled by qualified personnel only, trained in laboratory procedures.
References
1. Saito, A., et al. "A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors." Proc. Natl. Acad. Sci. USA 96:4592-4597 (1999). 2. Lee, B.I., et al. "MS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cells." Cancer Res. 61:931-934 (2001). 3. Eyüpoglu, I.Y., et al. "Experimental therapy of malignant gliomas using the inhibitor of histone deacetylase MS-275." Mol. Cancer Ther. 5:1248-1255 (2006). 4. Gojo, I., et al. "Phase 1 and pharmacologic study of MS-275, a histone deacetylase inhibitor, in adults with refractory and relapsed acute leukemias." Blood 109:2781-2790 (2007). 5. Lin, H.S., et al. "Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents." Br. J. Pharmacol. 150:862-872 (2007). 6. Khandelwal, A., et al. "MS-275 synergistically enhances the growth inhibitory effects of RAMBA VN/66-1 in hormone-insensitive PC-3 prostate cancer cells and tumours." Br. J. Cancer 98:1234-1243 (2008).
USBio References
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