| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
Amcasertib (formerly known as BBI-503; BBI503) is an orally bioavailable small molecule compound and a first-in-class cancer stemness kinase inhibitor. It was designed to target CSC (Cancer Stem Cell) pathways in multiple tumour types. As the first cancer stemness kinase inhibitor, it is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity. In a phase I study, BI503 as a monotherapy was tolerated at the recommended phase 2 dose of 300 mg once daily. At the recommended phase 2 dose, common adverse events were grade 1 to 2 diarrhea, nausea, abdominal cramping, anorexia and fatigue, and grade 3 adverse events were fatigue (n= 4), and diarrhea, nausea, and weight loss (n=1 each).
| ln Vitro |
In PC-9/GR cells, amcasertib (0-1μM; 48h) inhibits the expression of CD133 and NANOG. Additionally, in a dose-dependent manner, amcasertib significantly inhibits the growth of PC-9/GR cells[1].
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| ln Vivo |
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: PC-9/GR cell Tested Concentrations: 0, 0.3125, 0.625, 1.25, 2.5, 5 and 10μM Incubation Duration: 48 hrs (hours) Experimental Results: Suppressed the growth of PC-9/GR cells in a dose-dependent manner for 48 hrs (hours) with a OD value diminished from over 1.5 to less than 0.2 (p< 0.0001). Western Blot Analysis[1] Cell Types: PC-9/GR cell Tested Concentrations: 0, 0.1 and 1μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited the NANOG and CD133 expression in PC-9/GR cells. |
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| Animal Protocol |
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| References | |||
| Additional Infomation |
Amcasertib is under investigation in clinical trial NCT02483247 (A Study of BBI503 in Combination With Selected Anti-Cancer Therapeutics in Adult Patients With Advanced Cancer).
Amcasertib is an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity. Even though the exact target has not been fully elucidated, amcasertib targets and inhibits one or more pathways involved in cancer stem cell survival. As a result, cancer stem cell (CSC) growth as well as heterogeneous cancer cell growth is inhibited. CSCs, self-replicating cells able to differentiate into heterogeneous cancer cells, appear to be responsible for both tumor relapse and metastasis. |
| Molecular Formula |
C31H33N5O2S
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| Molecular Weight |
539.69
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| Exact Mass |
539.235
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| CAS # |
1129403-56-0
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| Related CAS # |
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| PubChem CID |
25190990
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.651
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| LogP |
5.72
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
39
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| Complexity |
888
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(C2C([H])=C([H])C([H])=C([H])C=2[H])=NC(=C1[H])C1C([H])=C([H])C2=C(C=1[H])/C(/C(N2[H])=O)=C(/[H])\C1=C(C([H])([H])[H])C(C(N([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)=C(C([H])([H])[H])N1[H]
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| InChi Key |
QDWKGEFGLQMDAM-ULJHMMPZSA-N
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| InChi Code |
InChI=1S/C31H33N5O2S/c1-5-36(6-2)15-14-32-30(38)28-19(3)26(33-20(28)4)17-24-23-16-22(12-13-25(23)34-29(24)37)27-18-39-31(35-27)21-10-8-7-9-11-21/h7-13,16-18,33H,5-6,14-15H2,1-4H3,(H,32,38)(H,34,37)/b24-17-
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| Chemical Name |
N-[2-(diethylamino)ethyl]-2,4-dimethyl-5-[(Z)-[2-oxo-5-(2-phenyl-1,3-thiazol-4-yl)-1H-indol-3-ylidene]methyl]-1H-pyrrole-3-carboxamide
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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: ≥ 1.25 mg/mL (2.32 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 12.5 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 | 1.8529 mL | 9.2646 mL | 18.5292 mL | |
| 5 mM | 0.3706 mL | 1.8529 mL | 3.7058 mL | |
| 10 mM | 0.1853 mL | 0.9265 mL | 1.8529 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.
Products are for research use only; We do not sell to patients
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