| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
With IC50 values of 0.147 μM for Lck and 9.1, 14.1, and 44.1 μM for Src, Fgr, and Fyn, respectively, A-770041 selectively inhibits these Src family kinases [1]. With an EC50 value of 80 nM, A-770041 (0-30 μM; 2 hours) dose-dependently suppresses anti-CD3-induced IL-2 production [1].
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|---|---|
| ln Vivo |
A-770041 (2.5 mg/kg; ig once) suppresses concanavalin A-induced IL-2 in vivo [1]. A-770041 (2.5-20 mg/kg/day; for 14 days) dosage-dependently enhanced survival at doses 5 and 10 mg/kg/day, and at dose 10, reached 100% survival before 20 mg/kg/day[1].
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| Animal Protocol |
Animal/Disease Models: Male Lewis rat [1]
Doses: 2.5 mg/kg Route of Administration: intragastric (po) (po)administration; 2.5 mg/kg Primary Experimental Results:demonstrated inhibitory effect on concanavalin A-induced IL-2, in vivo EC50 value is 78 nM. |
| References |
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| Additional Infomation |
N-[4-[1-[4-(4-acetyl-1-piperazinyl)cyclohexyl]-4-amino-3-pyrazolo[3,4-d]pyrimidinyl]-2-methoxyphenyl]-1-methyl-2-indolecarboxamide is an aromatic amide.
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| Molecular Formula |
C34H39N9O3
|
|---|---|
| Molecular Weight |
621.73196
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| Exact Mass |
621.318
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| CAS # |
869748-10-7
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| PubChem CID |
9549184
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| Appearance |
White to off-white solid powder
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| LogP |
5.316
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
46
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZMNWFTYYYCSSTF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C34H39N9O3/c1-21(44)41-14-16-42(17-15-41)24-9-11-25(12-10-24)43-33-30(32(35)36-20-37-33)31(39-43)23-8-13-26(29(19-23)46-3)38-34(45)28-18-22-6-4-5-7-27(22)40(28)2/h4-8,13,18-20,24-25H,9-12,14-17H2,1-3H3,(H,38,45)(H2,35,36,37)
|
| Chemical Name |
N-[4-[1-[4-(4-acetylpiperazin-1-yl)cyclohexyl]-4-aminopyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-1-methylindole-2-carboxamide
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~40.21 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.35 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (3.35 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 20.8 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: ≥ 2.08 mg/mL (3.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6084 mL | 8.0421 mL | 16.0842 mL | |
| 5 mM | 0.3217 mL | 1.6084 mL | 3.2168 mL | |
| 10 mM | 0.1608 mL | 0.8042 mL | 1.6084 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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