Silatecan

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

MedKoo CAT#: 200274

CAS#: 220913-32-6

Description: Silatecan (formerly AR-67) is a synthetic, highly lipophilic derivative of camptothecin, with potential antineoplastic and radiosensitizing activities. Silatecan DB-67 binds to and stabilizes the topoisomerase I-DNA covalent complex, inhibiting the religation of topoisomerase I-mediated single-stranded DNA breaks and producing lethal double-stranded DNA breaks when encountered by the DNA replication machinery; inhibition of DNA replication and apoptosis follow. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active lactone structure to an inactive carboxylate form.


Chemical Structure

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Silatecan
CAS# 220913-32-6

Theoretical Analysis

MedKoo Cat#: 200274
Name: Silatecan
CAS#: 220913-32-6
Chemical Formula: C26H30N2O5Si
Exact Mass: 478.1924
Molecular Weight: 478.61
Elemental Analysis: C, 65.25; H, 6.32; N, 5.85; O, 16.71; Si, 5.87

Price and Availability

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Synonym: AR67; AR 67; AR-67; DB67; DB 67; DB-67; 7-t-Butyl-dimethylsilyl-10-hydroxycamptothecin; Silatecan.

IUPAC/Chemical Name: (S)-11-(tert-butyldimethylsilyl)-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione

InChi Key: XUSKJHCMMWAAHV-SANMLTNESA-N

InChi Code: InChI=1S/C26H30N2O5Si/c1-7-26(32)18-11-20-21-16(12-28(20)23(30)17(18)13-33-24(26)31)22(34(5,6)25(2,3)4)15-10-14(29)8-9-19(15)27-21/h8-11,29,32H,7,12-13H2,1-6H3/t26-/m0/s1

SMILES Code: O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C([Si](C)(C(C)(C)C)C)C5=CC(O)=CC=C5N=C4C3=C2)=O

Appearance: white 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

Preparing Stock Solutions

The following data is based on the product molecular weight 478.61 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.

Recalculate based on batch purity %
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

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Additional Information

AR-67(DB-67) is a novel, third-generation camptothecin analogue that has demonstrated high potency in preclinical studies and improved pharmacokinetic properties in humans as compared with first and second-generation products. Arno believes that this unique profile and the potential for oral administration may translate into superior efficacy and patient convenience in the treatment of brain, lung, and other cancers. We believe these advantages could allow DB-67 to become a leading product in the $1.1 billion camptothecin market. Arno is currently conducting a single agent, ascending dose, Phase I clinical study of DB-67 in patients with advanced solid tumors. The study is evaluating the safety of DB-67, establishing the maximum tolerated dose, and characterizing the plasma PK profile.