[CAS NO. 151823-14-2] Sapacitabine
PRODUCTS SPECIFICATIONS [151823-14-2]
DESCRIPTION [151823-14-2]
Overview
| MDL | MFCD00919466 |
|---|---|
| Molecular Weight | 490.64 |
| Molecular Formula | C26H42N4O5 |
| SMILES | O=C(N=C(NC(CCCCCCCCCCCCCCC)=O)C=C1)N1[C@H]2[C@@H](C#N)[C@H](O)[C@@H](CO)O2 |
Summary
Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.
IC50 & Target
nucleoside analog [1]
In Vitro
Concentrations of Sapacitabine required to achieve an IC 50 range from 3±0.6 μM for the colon cancer cell line HCT116 to 67±14 μM for the breast cancer cell line MDA-MB-435. Cell cycle analysis shows that 35% Sapacitabine-treated cells are arrested in late-S phase and 41% in G 2 /M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC 50 20±6 μM). In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
On Day 14, the Sapacitabine (5 mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 245 mm 3 and a tumour growth inhibition (TGI) of 92%, whereas the Sapacitabine (15 mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 107 mm 3 and a TGI of 112% [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00999401 | Cyclacel Pharmaceuticals, Inc. |
Advanced Solid Tumors
|
April 2009 | Phase 1 |
| NCT00885963 | Cyclacel Pharmaceuticals, Inc. |
Non-small Cell Lung Cancer
|
December 1, 2008 | Phase 2 |
| NCT00476554 | Cyclacel Pharmaceuticals, Inc. |
Cutaneous T-cell Lymphoma (CTCL)
|
April 2007 | Phase 2 |
| NCT00380653 | Cyclacel Pharmaceuticals, Inc. |
Leukemias|Myelodysplastic Syndromes
|
January 2006 | Phase 1 |
| NCT01211457 | Cyclacel Pharmaceuticals, Inc.|M.D. Anderson Cancer Center |
Acute Myeloid Leukemia|Myelodysplastic Syndromes
|
June 17, 2010 | Phase 1|Phase 2 |
| NCT01303796 | Cyclacel Pharmaceuticals, Inc. |
Acute Myeloid Leukemia
|
October 1, 2011 | Phase 3 |
| NCT03641755 | Dana-Farber Cancer Institute|AstraZeneca|Cyclacel Pharmaceuticals, Inc. |
Breast Cancer
|
October 1, 2018 | Phase 1 |
| NCT01253460 | M.D. Anderson Cancer Center|Cyclacel Pharmaceuticals, Inc.|National Cancer Institute (NCI) |
Leukemia
|
August 22, 2011 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 67.93 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0382 mL | 10.1908 mL | 20.3815 mL |
| 5 mM | 0.4076 mL | 2.0382 mL | 4.0763 mL |
| 10 mM | 0.2038 mL | 1.0191 mL | 2.0382 mL |
References
- [1] Serova M, et al. Antiproliferative effects of sapacitabine (CYC682), a novel 2'-deoxycytidine-derivative, in human cancer cells. Br J Cancer. 2007 Sep 3;97(5):628-36.
- [2] Green SR, et al. Combination of sapacitabine and HDAC inhibitors stimulates cell death in AML and other tumour types. Br J Cancer. 2010 Oct 26;103(9):1391-9.
Synonyms