| Size | Price | Stock | Qty |
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| 250mg |
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Purity: ≥98%
Bicalutamide (formerly known as ICI-176334; CDX; trade names: Casodex in the USA and Cosudex in other countries), a marketed drug for treating PC (prostate cancer), is a potent, synthetic, nonsteroidal androgen receptor (AR) antagonist with potential anticancer activity. It inhibits AR with an IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide inhibits the growth of prostate cancer cells which overexpress androgen receptor by directly binding to AR then mediates androgen-mediated gene transcription. Bicalutamide directly binds to androgen receptor with Ki value of 12.5μM. In prostate cancer cells, bicalutamide impairs DNA binding and nuclear localization. Bicalutamide and MDV3100 significantly inhibited R1881-induced VP16-AR–mediated transcription in HepG2 cells with an IC50 value of 0.2 μM.
| ln Vitro |
Bicalutamide has an IC50 of 160 nM and competes with androgens for binding to AR in a whole-cell binding experiment (LNCaP/AR (cs) cells) [1]. Bicalutamide partially counteracts the effects of R1881, a synthetic androgen, while inducing VCaP cell proliferation in a dose-dependent manner [1].
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| ln Vivo |
In a mouse model of prostate cancer, belicutamide (10 mg/kg; ig; daily; for 28 days) shows anticancer efficacy [1].
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| Animal Protocol |
Animal/Disease Models: Castrate male mice, bearing LNCaP/AR(cs) xenograft tumors[1]
Doses: 10 mg/kg Route of Administration: po (oral gavage), daily, for 28 days Experimental Results: Inhibited tumor growth. |
| References |
[1]. Nicola J. Clegg,1 John Wongvipat,1,2 Jim Joseph, ARN-509: a novel anti-androgen for prostate cancer treatment. Cancer Res. 2012 March 15; 72(6): 1494-1503.
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| Molecular Formula |
C18H14F4N2O4S
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|---|---|
| Molecular Weight |
430.37
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| CAS # |
90357-06-5
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| Related CAS # |
(R)-Bicalutamide;113299-40-4;Bicalutamide-d4;1185035-71-5
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| SMILES |
O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)C(C)(O)CS(=O)(C2=CC=C(F)C=C2)=O
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| InChi Key |
LKJPYSCBVHEWIU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
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| Chemical Name |
N-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
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| Synonyms |
ICI-176334; ICI 176334; ICI176334; CDX. US trade name: Casodex; Cosudex.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3236 mL | 11.6179 mL | 23.2358 mL | |
| 5 mM | 0.4647 mL | 2.3236 mL | 4.6472 mL | |
| 10 mM | 0.2324 mL | 1.1618 mL | 2.3236 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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