| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
A-443654 is 30,000 times more potent than the original lead molecule, with a Ki value of 160 pM. Compared to PKA, A-443654 has 40 times more selectivity for Akt. In cells, A-443654 inhibits Akt1, Akt2, or Akt3 in an equal manner. In all three cell lines, A-443654 lowered P-GSK3 in a dose-responsive way. At an EC50 of 0.1 μM, A-443654 suppresses the growth of tumor cells[1]. A-443654 caused morphological alterations in 10A and 10CA1a cells relatively quickly (in 2 to 4 hours), with 10CA1a cells being more sensitive to A-443654 than 10A cells. After 12 hours, A-443654 at 2 μM alone induced 10CA1a cells to separate from the plate, but not 10A cells. At 1 μM, on the other hand, 10CA1a cells separated from the plate. Rapamycin and A-443654's effects on the DNA content of 10A and 10CA1a cells were examined using FACScan. Conversely, after 8 hours, A-443654 at 2 and 5 μM decreased Bcl-2 levels in 10CA1a cells by 30% to 40%. Rapamycin and 2 or 5 μM A-443654 together, however, dramatically decreased Bcl-2 protein levels by around 40% to 50% in 10A cells and about 70% in 10CA1a cells [2]. A-443654 exhibits a relative growth inhibition of more than 3.5 times on mutant cells, which is the largest selective effect on mutant cells when compared to WT cells [3].
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| ln Vivo |
In the 3T3-Akt1 flank tumor model, subcutaneous administration of A-443654 (7.5 mg/kg/d) suppresses tumor growth. A-443654 (50 mg/kg, subcutaneously) causes the tumor cells around 3T3-Akt1 to undergo apoptosis. In MiaPaCa-2 tumors, A-443654 (30 mg/kg, subcutaneous injection) raises phosphorylated Akt1 levels [1].
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| References |
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| Additional Infomation |
(2S)-1-(1H-indol-3-yl)-3-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-2-propanamine is a member of indoles.
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| Exact Mass |
397.19
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|---|---|
| CAS # |
552325-16-3
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| PubChem CID |
10172943
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
722.0±60.0 °C at 760 mmHg
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| Flash Point |
390.4±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.722
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| LogP |
3.65
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
562
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| Defined Atom Stereocenter Count |
1
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| SMILES |
N[C@H](COC1=CN=CC(C2=CC3=C(NN=C3C)C=C2)=C1)CC4=CNC5=CC=CC=C54
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| InChi Key |
YWTBGJGMTBHQTM-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C24H23N5O/c1-15-22-10-16(6-7-24(22)29-28-15)17-9-20(13-26-11-17)30-14-19(25)8-18-12-27-23-5-3-2-4-21(18)23/h2-7,9-13,19,27H,8,14,25H2,1H3,(H,28,29)/t19-/m0/s1
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| Chemical Name |
(2S)-1-(1H-indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan-2-amine
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| Synonyms |
A443564 A 443564 A-443564
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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 (~251.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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