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Purity: ≥98%
BMS-833923 (also known as XL139; BMS833923; XL-139; BMS 833923) is a novel, potent, selective, and orally bioavailable inhibitor of SMO (Smoothened) with potential antineoplastic activity. It inhibits the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC50 of 21 nM. BMS-833923 suppresses the sonic hedgehog (SHH) signaling pathway by inhibiting the SMO protein of the SHH pathway. Using a single oral dose, BMS-833923 effectively inhibits the activity of the HH pathway in xenograft models of pancreatic cancer and medulloblastoma.
| Targets |
Smoothened
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| ln Vitro |
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| Enzyme Assay |
BMS-833923 (also known as XL-139) is a potentially antineoplastic small-molecule inhibitor that can be taken orally. Its IC50 is 21 nM, and it inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner.
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| Cell Assay |
BMS-833923 suppressed the expression of GLI1 and PTCH1 in cell lines that expressed activated mutant SMO or wild-type SMO, with IC50 values ranging from 6 to 35 nM. It does-dependently inhibit cyclopamine binding to SMO in the FACS-based binding assays, with an IC50 value of 21 nM. With IC50 values of 10 μM, BMS-833923 treatment markedly decreased cell proliferation in the esophageal adenocarcinoma cell lines OE19 and OE33. In addition, BMS-833923 was discovered to suppress the percentage of ALDH+ cancer stem cells as well as the proliferation of multiple myeloma cells. Numerous additional tumor cells grown from patients with hematological malignancies, such as ALL, AML, and CM, were also inhibited in growth by it.
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| References |
| Molecular Formula |
C30H27N5O
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| Molecular Weight |
473.57
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| Exact Mass |
473.22
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| Elemental Analysis |
C, 76.09; H, 5.75; N, 14.79; O, 3.38
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| CAS # |
1059734-66-5
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| Appearance |
White solid powder
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| SMILES |
CC1=C(C=C(C=C1)CNC)NC(=O)C2=CC=C(C=C2)NC3=NC4=CC=CC=C4C(=N3)C5=CC=CC=C5
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| InChi Key |
KLRRGBHZCJLIEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H27N5O/c1-20-12-13-21(19-31-2)18-27(20)33-29(36)23-14-16-24(17-15-23)32-30-34-26-11-7-6-10-25(26)28(35-30)22-8-4-3-5-9-22/h3-18,31H,19H2,1-2H3,(H,33,36)(H,32,34,35)
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| Chemical Name |
N-[2-methyl-5-(methylaminomethyl)phenyl]-4-[(4-phenylquinazolin-2-yl)amino]benzamide
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| Synonyms |
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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 |
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| 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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1116 mL | 10.5581 mL | 21.1162 mL | |
| 5 mM | 0.4223 mL | 2.1116 mL | 4.2232 mL | |
| 10 mM | 0.2112 mL | 1.0558 mL | 2.1116 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00909402 | Completed | Drug: BMS-833923 Drug: Cisplatin |
Stomach Neoplasms Esophageal Neoplasms |
Bristol-Myers Squibb | November 2009 | Phase 1 |
| NCT01218477 | Completed | Drug: Dasatinib Drug: BMS-833923 |
Leukemia | Bristol-Myers Squibb | January 2011 | Phase 1 Phase 2 |
| NCT00670189 | Completed | Drug: BMS-833923 (XL139) | Hedgehog Pathway Smoothened |
Bristol-Myers Squibb | July 2008 | Phase 1 |
| NCT01413906 | Completed | Drug: BMS-833923 (XL139) | Cancer | Bristol-Myers Squibb | November 2011 | Phase 1 |
| NCT02100371 | Completed | Drug: BMS-833923 | Basal Cell Nevus Syndrome | University Health Network, Toronto |
February 2014 | Not Applicable |
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