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CPI203 - 98% (HPLC), high purity , CAS No.1446144-04-2, Inhibitor of bromodomain containing 4

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CPI203 - 98% (HPLC), high purity , CAS No.1446144-04-2, Inhibitor of bromodomain containing 4

Moligand™

≥98%(HPLC)

CAS#: 1446144-04-2
Molecular Weight: 399.9
MDL number: MFCD27997886
PubChem CID: 71291068
PubChem SID: 504772011

In stock

Item Number

C167316

Grouped product items
SKU	Size	Availability	Price
C167316-5mg	5mg	9	$129.90
C167316-25mg	25mg	6	$521.90
C167316-100mg	100mg	6	$1,879.90

BET bromodomain inhibitor; arrests cell cycle at G1phase

View related series

bromodomain containing 4 Inhibitor (42) Epigenetic Reader Domain (260) Epigenetics (1500)

Basic Description

Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	BET bromodomain inhibitor. Downregulates Myc expression, causes G1cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. Arrests the growth of T cell acute lymphoblastic leukemia cellsin vitro(EC50= 91.2 nM). Also e
Storage Temp	Store at 2-8°C
Shipped In	Wet ice
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of bromodomain containing 4
Product Description	CPI203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.

Associated Targets(Human)

BRD4 Tchem Bromodomain-containing protein 4 (2 Activities)

Discover Target: BRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HepG2 (196354 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)

Discover Target: BRD4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)

Discover Target: Hdac6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

rep Replicase polyprotein 1ab (378 Activities)

Discover Target: rep

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mechanisms of Action

Mechanism of Action	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	References

Names and Identifiers

Pubchem Sid	504772011
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/504772011
IUPAC Name	2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetamide
INCHI	InChI=1S/C19H18ClN5OS/c1-9-10(2)27-19-16(9)17(12-4-6-13(20)7-5-12)22-14(8-15(21)26)18-24-23-11(3)25(18)19/h4-7,14H,8H2,1-3H3,(H2,21,26)/t14-/m0/s1
InChi Key	QECMENZMDBOLDR-AWEZNQCLSA-N
Canonical SMILES	CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)N)C4=CC=C(C=C4)Cl)C
Isomeric SMILES	CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)N)C4=CC=C(C=C4)Cl)C
PubChem CID	71291068
Molecular Weight	399.9

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

2 results found

Lot Number	Certificate Type	Date	Item
F2002054	Certificate of Analysis	Mar 13, 2023	C167316
L2220186	Certificate of Analysis	Jan 06, 2023	C167316

Chemical and Physical Properties

Solubility	Solvent:DMSO, Max Conc. mg/mL: 39.99, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 4, Max Conc. mM: 10
Molecular Weight	399.900 g/mol
XLogP3	2.900
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	3
Exact Mass	399.092 Da
Monoisotopic Mass	399.092 Da
Topological Polar Surface Area	114.000 Å²
Heavy Atom Count	27
Formal Charge	0
Complexity	611.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

Specifications

Specification Sheet

References

1. Moros A, Rodríguez V, Saborit-Villarroya I, Montraveta A, Balsas P, Sandy P, Martínez A, Wiestner A, Normant E, Campo E et al.. (2014) Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma.. Leukemia, 28 (10): (2049-59). [PMID:24721791] [10.1021/op500134e]
2. Wong C, Laddha SV, Tang L, Vosburgh E, Levine AJ, Normant E, Sandy P, Harris CR, Chan CS, Xu EY. (2014) The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors.. Cell Death Dis, 5 (13): (e1450). [PMID:25299775] [10.1021/op500134e]

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