Briciclib | ON-013105 | CAS#865783-99-9 | CAS#865784-01-6 | benzyl styryl sulfone analog

Briciclib
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205563

CAS#: 865783-99-9 (free acid)

Description: Briciclib, also known as ON 013105 or ON 014185, is a benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity. Upon hydrolysis, cyclin D modulator ON 013105 is converted to ON 013100, which blocks cyclin D mRNA translation and decreases protein expression of cyclin D. This may induce cell cycle arrest and apoptosis in cancer cells overexpressing cyclin D and eventually decrease tumor cell proliferation. This agent may exhibit synergistic antitumor activity in combination with other chemotherapeutic agents.

Chemical Structure

Briciclib

CAS# 865783-99-9 (free acid)

Instruction

Theoretical Analysis

MedKoo Cat#: 205563
Name: Briciclib
CAS#: 865783-99-9 (free acid)
Chemical Formula: C19H23O10PS
Exact Mass: 474.08
Molecular Weight: 474.417
Elemental Analysis: C, 48.10; H, 4.89; O, 33.72; P, 6.53; S, 6.76

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 190
25mg	USD 350
50mg	USD 550
100mg	USD 850
200mg	USD 1450
500mg	USD 2150
1g	USD 3250
2g	USD 4850
5g	USD 7450
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 865784-01-6 (Na); 865783-99-9 (free acid)

Synonym: ON013105; ON-013105; ON 013105; ON 014185; ON014185; ON-014185; ON-013105 sodium, Briciclib.

IUPAC/Chemical Name: (E)-2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl dihydrogen phosphate

InChi Key: LXENKEWVEVKKGV-BQYQJAHWSA-N

InChi Code: InChI=1S/C19H23O10PS/c1-25-14-10-17(27-3)15(18(11-14)28-4)7-8-31(23,24)12-13-5-6-16(26-2)19(9-13)29-30(20,21)22/h5-11H,12H2,1-4H3,(H2,20,21,22)/b8-7+

SMILES Code: O=P(O)(O)OC1=CC(CS(=O)(/C=C/C2=C(OC)C=C(OC)C=C2OC)=O)=CC=C1OC

Appearance: Solid powder

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

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

More Info: Related: 865783-99-9 (Briciclib free acid) 865784-01-6 (Briciclib disodium salt). ON-013105 is a new chemical entity, currently in Phase I clinical development, which targets cyclin D1 overexpression. It exhibits selective effects on cell cycle progression in malignant tumor cells driving them into apoptosis following mitotic arrest, whereas, normal healthy cells are not arrested in mitosis by ON 013105.

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 474.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1. Prasad A, Shrivastava A, Papadopoulos E, Kuzontkoski PM, Reddy MV, Gillum AM, Kumar R, Reddy EP, Groopman JE. Combined administration of rituximab and on 013105 induces apoptosis in mantle cell lymphoma cells and reduces tumor burden in a mouse model of mantle cell lymphoma. Clin Cancer Res. 2013 Jan 1;19(1):85-95. doi: 10.1158/1078-0432.CCR-12-1425. Epub 2012 Nov 1. PubMed PMID: 23124440.

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