| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| ln Vitro |
PC3 cell proliferation is inhibited by estramustine sodium phosphate (1 µg/mL, 48 hours) [1]. By decreasing miR-31, estramustine sodium phosphate (2 µg/mL, 48 h) can cause PC3 cells to undergo more phosphatidylserine eversion and ultimately undergo apoptosis [1]. In RAW 264.7 cells, estramustine sodium phosphate (0–40 µM, 24-72 hours) suppresses tubulin cytoskeleton and cell growth [2]. By blocking Smad3 activation, estramustine sodium phosphate (10 µM, 24 hours) prevents TGF-β-induced RAW 264.7 cell migration and TGF-β-induced uPA generation [2].
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|---|---|
| ln Vivo |
Estramustine sodium phosphate (ip, 4 or 12 mg/kg daily for 2 weeks) reduced PAC120 tumor growth by 53% on day 35 [3].
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| Cell Assay |
Cell viability assay [1]
Cell Types: PC3 Cell Tested Concentrations: 1 µg/mL Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of PC3 cell growth. Immunofluorescence[2] Cell Types: RAW 264.7 Cell Tested Concentrations: 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: Disruption of interphase microtubules. Cell migration assay[2] Cell Types: RAW 264.7 cells treated with TGF-β for 18 hrs (hours) Tested Concentrations: 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of TGF-β induced cell migration. |
| Animal Protocol |
Animal/Disease Models: Swiss nu/nu (nude) male mice (5 weeks old) with PAC120 tumors [3]
Doses: 4 mg/kg, 12 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; for 2 weeks Experimental Results: Inhibition of skin lesion development and resulting dissociation between DTH response and antibody production. Animal/Disease Models: Human Prostate Cancer Xenograft PAC120[3] Doses: 4 or 12 mg/kg daily for 2 weeks. Route of Administration: intraperitoneal (ip) injection. Experimental Results: On day 35, PAC120 inhibited tumor growth by 53%. |
| References |
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| Additional Infomation |
Estramustine sodium phosphate is an organic sodium salt which is the disodium salt of estramustine phosphate. It contains an estramustine phosphate(2-).
Estramustine Phosphate Sodium is the orally available disodium salt, monohydrate, of estramustine phosphate, a synthetic molecule that combines estradiol and nornitrogen mustard through a carbamate link. Estramustine and its major metabolite estramustine bind to microtubule-associated proteins (MAPs) and tubulin, thereby inhibiting microtubule dynamics and leading to anaphase arrest in a dose-dependent fashion. This agent also exhibits anti-androgenic effects. A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties. See also: Estramustine (has active moiety). |
| Exact Mass |
563.098
|
|---|---|
| CAS # |
52205-73-9
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| Related CAS # |
Estramustine phosphate;4891-15-0
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| PubChem CID |
444000
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| Appearance |
White to off-white solid powder
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| Density |
1.253g/cm3
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| Boiling Point |
565.8ºC at 760mmHg
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| Flash Point |
296ºC
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| LogP |
6.175
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
|
| Heavy Atom Count |
35
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| Complexity |
735
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| Defined Atom Stereocenter Count |
5
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| SMILES |
[O-]P([O-])(O[C@H]1CC[C@@]2([H])[C@@]3([H])[C@](C(C=CC(OC(N(CCCl)CCCl)=O)=C4)=C4CC3)([H])CC[C@@]21C)=O.[Na+].[Na+]
|
| InChi Key |
IIUMCNJTGSMNRO-VVSKJQCTSA-L
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| InChi Code |
InChI=1S/C23H32Cl2NO6P.2Na/c1-23-9-8-18-17-5-3-16(31-22(27)26(12-10-24)13-11-25)14-15(17)2-4-19(18)20(23)6-7-21(23)32-33(28,29)30;;/h3,5,14,18-21H,2,4,6-13H2,1H3,(H2,28,29,30);;/q;2*+1/p-2/t18-,19-,20+,21+,23+;;/m1../s1
|
| Chemical Name |
disodium;[(8R,9S,13S,14S,17S)-3-[bis(2-chloroethyl)carbamoyloxy]-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] phosphate
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| Synonyms |
EmcytRo 21-8837/001 Leo299 estramustine Phosphate sodium EstracytRo 222296000 LS 299 NSC 89199
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~62.5 mg/mL (~110.75 mM)
DMSO : ~5 mg/mL (~8.86 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 65 mg/mL (115.18 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00003066 | UNKNOWN STATUS | Drug: docetaxel Drug: estramustine phosphate sodium |
Breast Cancer | Herbert Irving Comprehensive Cancer Center | 1997-02 | Phase 2 |
| NCT00025194 | COMPLETED | Drug: estramustine phosphate sodium Drug: ixabepilone |
Prostate Cancer | Memorial Sloan Kettering Cancer Center | 2001-07 | Phase 1 Phase 2 |
| NCT00004105 | COMPLETED | Drug: estramustine phosphate sodium Drug: paclitaxel Drug: vinorelbine ditartrate |
Leukemia Lymphoma Sarcoma Unspecified Adult Solid Tumor, Protocol Specific |
NYU Langone Health | 1998-09 | Phase 1 Phase 2 |
| NCT00021372 | COMPLETED | Drug: estramustine phosphate sodium Drug: paclitaxel |
Lymphoma | Fox Chase Cancer Center | 1996-02 | Phase 2 |
| NCT00002775 | UNKNOWN STATUS | Drug: docetaxel Drug: estramustine phosphate sodium |
Prostate Cancer | Herbert Irving Comprehensive Cancer Center | 1998-02 | Phase 1 Phase 2 |
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