| 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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| Other Sizes |
Purity: ≥98%
| 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].
In PC-9/GR (gefitinib-resistant non-small cell lung cancer) cells, treatment with Amcasertib (BBI503) at concentrations of 0.1 and 1 μmol/L for 48 hours inhibited the expression of NANOG and CD133, as determined by western blotting [1]. Treatment with Amcasertib at indicated concentrations for 48 hours suppressed the growth of PC-9/GR cells in a dose-dependent manner [1]. Combined treatment with Amcasertib (0.1 μM) and gefitinib significantly decreased the IC50 value against gefitinib in PC-9/GR cells compared to gefitinib alone [1]. |
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| ln Vivo |
Amcasertib inhibits Nanog and other cancer stem cell pathways by targeting kinases, and shows encouraging early signs of anti-cancer activity for patients with advanced colorectal cancer.
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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. The detailed experimental procedure for Amcasertib was not described in the provided manuscript [1]. |
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| Animal Protocol |
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| References | |||
| Additional Infomation |
Amcasertib is being investigated in the clinical trial NCT02483247 (a study of BBI503 in combination with specific anticancer therapies for adult patients with advanced cancer). Amcasertib is an orally administered cancer stem cell kinase inhibitor with potential antitumor activity. Although its exact target is not fully elucidated, Amcasertib targets and inhibits one or more pathways associated with cancer stem cell survival. Therefore, the growth of cancer stem cells (CSCs) and heterogeneous cancer cells is suppressed. CSCs are cells capable of self-replication and differentiation into heterogeneous cancer cells, and appear to be the culprits behind tumor recurrence and metastasis.
Amcasertib (BBI503) is a small-molecule multi-kinase inhibitor [1]. It was used in combination with gefitinib to evaluate its effect on cancer stem-like properties and gefitinib resistance in NSCLC cells [1]. |
| 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 |
Light yellow to yellow solid powder
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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.
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