CPI203
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MedKoo CAT#: 407122

CAS#: 1446144-04-2

Description: CPI203, also known as TEN010, JQ-2; RO6870810 and RG6146, is a potent and orally active BET bromodomain inhibitor. CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. CPI203 ownregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. CPI203 arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM).


Price and Availability

Size Price Shipping out time Quantity
10mg USD 190 Same day
25mg USD 350 Same day
50mg USD 550 Same day
100mg USD 950 Same day
200mg USD 1650 Same day
500mg USD 2450 Same day
1g USD 3250 2 Weeks
2g USD 3950 2 Weeks
5g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-26. Prices are subject to change without notice.

CPI203, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407122
Name: CPI203
CAS#: 1446144-04-2
Chemical Formula: C19H18ClN5OS
Exact Mass: 399.09206
Molecular Weight: 399.9
Elemental Analysis: C, 57.07; H, 4.54; Cl, 8.86; N, 17.51; O, 4.00; S, 8.02


Synonym: CPI203; CPI-203; CPI 203; TEN010; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RG 6146; RG-6146; RO6870810; RO-6870810; RO 6870810

IUPAC/Chemical Name: (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide

InChi Key: QECMENZMDBOLDR-AWEZNQCLSA-N

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

SMILES Code: O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

TEN-010 binds to the acetylated lysine recognition motifs found in the bromodomain of BET proteins, which prevents the interaction between BET proteins and acetylated histones. This interaction disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth.


References

1: Wong C, Laddha SV, Tang L, Vosburgh E, Levine AJ, Normant E, Sandy P, Harris CR, Chan CS, Xu EY. The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. Cell Death Dis. 2014 Oct 9;5:e1450. doi: 10.1038/cddis.2014.396. PubMed PMID: 25299775; PubMed Central PMCID: PMC4237236.

2: Moros A, Rodríguez V, Saborit-Villarroya I, Montraveta A, Balsas P, Sandy P, Martínez A, Wiestner A, Normant E, Campo E, Pérez-Galán P, Colomer D, Roué G. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. Leukemia. 2014 Oct;28(10):2049-59. doi: 10.1038/leu.2014.106. Epub 2014 Mar 18. PubMed PMID: 24721791.