Synonym
DRF-1042; DRF 1042; DRF1042; 5-(2'-Hydroxyethoxy)-20(S)-camptothecin.
IUPAC/Chemical Name
(4S)-4-ethyl-4-hydroxy-12-(2-hydroxyethoxy)-1,12-dihydro-14H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H)-dione
InChi Key
XAKLYHGHEFMDAP-IAXKEJLGSA-N
InChi Code
InChI=1S/C22H20N2O6/c1-2-22(28)15-10-17-18-13(9-12-5-3-4-6-16(12)23-18)20(29-8-7-25)24(17)19(26)14(15)11-30-21(22)27/h3-6,9-10,20,25,28H,2,7-8,11H2,1H3/t20?,22-/m0/s1
SMILES Code
O=C1[C@](O)(CC)C2=C(CO1)C(N3C(OCCO)C4=CC5=CC=CC=C5N=C4C3=C2)=O
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
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
408.41
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 |
1: Chatterjee A, Digumarti R, Katneni K, Upreti VV, Mamidi RN, Mullangi R, Surath
A, Srinivas ML, Uppalapati S, Jiwatani S, Srinivas NR. Safety, tolerability, and
pharmacokinetics of a capsule formulation of DRF-1042, a novel camptothecin
analog, in refractory cancer patients in a bridging phase I study. J Clin
Pharmacol. 2005 Apr;45(4):453-60. PubMed PMID: 15778426.
2: Chatterjee A, Digumarti R, Mamidi RN, Katneni K, Upreti VV, Surath A, Srinivas
ML, Uppalapati S, Jiwatani S, Subramaniam S, Srinivas NR. Safety, tolerability,
pharmacokinetics, and pharmacodynamics of an orally active novel camptothecin
analog, DRF-1042, in refractory cancer patients in a phase I dose escalation
study. J Clin Pharmacol. 2004 Jul;44(7):723-36. PubMed PMID: 15199077.
3: Upreti VV, Mamidi RN, Katneni K, Srinivas NR. Quantitative determination of
DRF-1042 in human plasma by HPLC: validation and application in clinical
pharmacokinetics. Biomed Chromatogr. 2003 Sep;17(6):385-90. PubMed PMID:
13680849.
