A bioavailable inhibitor of BET bromodomains
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CPI-203

Item No. 15479

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
CAS Number
1446144-04-2
Molecular Formula
C19H18ClN5OS
Formula Weight
399.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 20 mg/ml
λmax
255 nm
SMILES
ClC1=CC=C(C=C1)C2=N[C@@H](CC(N)=O)C3=NN=C(C)N3C4=C2C(C)=C(C)S4
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    (+)-JQ1 (Item No. 11187) binds to the acetyl-lysine recognition pocket of bromodomains 1 and 2 on BRD4 with Kd values of ~50 and 90 nM, respectively.1 This displaces BRD4 from nuclear chromatin in cells, inducing differentiation and growth arrest in midline carcinoma cells.1 CPI-203 is a primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration.2 It is comparable or superior to (+)-JQ1 in inhibiting BRD4 binding and action in vitro or in cells.2,3 CPI-203 arrests the growth of leukemic T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Filippakopoulos, P., Qi, J., Picaud, S., et al. Selective inhibition of BET bromodomains. Nature 468(7327), 1067-1073 (2010).

    2. King, B., Trimarchi, T., Reavie, L., et al. The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability. Cell 153(7), 1552-1566 (2013).

    3. Devaiah, B.N., Leiw, B.A., Cherman, N., et al. BRD4 is an atypical kinase that phosphorylates serine 2 of the RNA polymerase II carboxy-terminal domain. Proc. Natl. Acad. Sci. USA 109(18), 6927-6932 (2012).