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5mg |
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25mg |
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50mg |
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100mg |
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500mg |
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Purity: ≥98%
Fostemsavir (BMS-663068; BMS663068; Rukobia), the phosphonooxymethyl prodrug of BMS-626529, is an approved (in 2020) antiretroviral medication for adults living with HIV/AIDS. It is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells. The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. In order to better understand the anti-HIV-1 spectrum of BMS-626529 against HIV-1, in vitro activities against a wide variety of laboratory strains and clinical isolates were determined. BMS-626529 had half-maximal effective concentration (EC(50)) values of lt 10 nm against the vast majority of viral susceptibility varied by gt 6 log(10), with half-maximal effective concentration values in the low pM range against the most susceptible viruses. The in vitro antiviral activity of BMS-626529 was generally not associated with either tropism or subtype, with few exceptions. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life. Finally, in two-drug combination studies, BMS-626529 demonstrated additive or synergistic interactions with antiretroviral drugs of different mechanistic classes. These results suggest that BMS-626529 should be active against the majority of HIV-1 viruses and support the continued clinical development of the compound.
Targets |
HIV-1
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ln Vivo |
BMS-663068, also known as fostemsavir, demonstrates strong antiviral activity against subjects harboring virus infection and IC50 values less than 100 nM[1].
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References |
Molecular Formula |
C25H26N7O8P
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Molecular Weight |
583.48984
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Exact Mass |
583.16
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Elemental Analysis |
C, 51.46; H, 4.49; N, 16.80; O, 21.94; P, 5.31
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CAS # |
864953-29-7
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Related CAS # |
Temsavir;701213-36-7;Fostemsavir Tris;864953-39-9
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Appearance |
Solid powder
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SMILES |
CC1=NN(C=N1)C2=NC=C(C3=C2N(C=C3C(=O)C(=O)N4CCN(CC4)C(=O)C5=CC=CC=C5)COP(=O)(O)O)OC
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InChi Key |
SWMDAPWAQQTBOG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C25H26N7O8P/c1-16-27-14-32(28-16)23-21-20(19(39-2)12-26-23)18(13-31(21)15-40-41(36,37)38)22(33)25(35)30-10-8-29(9-11-30)24(34)17-6-4-3-5-7-17/h3-7,12-14H,8-11,15H2,1-2H3,(H2,36,37,38)
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Chemical Name |
(3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-1-yl)methyl dihydrogen phosphate
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Synonyms |
BMS-663068; BMS663068; BMS-663068 dihydrate; BMS 663068; Fostemsavir
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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 |
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) |
DMSO : ~100 mg/mL ( ~171.38 mM )
H2O : ~20 mg/mL (~34.28 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 8.33 mg/mL (14.28 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7138 mL | 8.5691 mL | 17.1383 mL | |
5 mM | 0.3428 mL | 1.7138 mL | 3.4277 mL | |
10 mM | 0.1714 mL | 0.8569 mL | 1.7138 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.
(A) Distribution of EC50s for BMS-626529 against HIV-1 subtype B clinical isolates in the PBMC assay.Antimicrob Agents Chemother.2012 Jul;56(7):3498-507. th> |
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Distribution of EC50s for BMS-626529 against HIV-1 non-subtype B clinical isolates in the PBMC assay.Antimicrob Agents Chemother.2012 Jul;56(7):3498-507. td> |
Distribution of EC50s for BMS-626529 against HIV-1 clinical isolates according to tropism in the PBMC assay.Antimicrob Agents Chemother.2012 Jul;56(7):3498-507. td> |