| 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 |
For AML cell lines and FLT3-ITD-positive AML cell lines, rohinitib (6.25–50 nM; 72 h) causes cell apoptosis[1]. Normal bone marrow (BM) is less sensitive to Rohinitib (25 nM; 72 h) than primary AML cells, and FLT3-ITD-positive cells are more sensitive than FLT3 wild-type AML cells[1].
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|---|---|
| ln Vivo |
In vivo, rohinitib (0.75 and 1.0 mg/kg; sc once daily for 5 days until mice get moribund) exhibits anti-AML effects[1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: AML cell lines Tested Concentrations: 6.25, 12.5, 25 and 50 nM Incubation Duration: 72 h Experimental Results: Dose-dependently induced apoptosis of MOLM-13, MOLM-14, MV4;11, OCI-AML3, THP-1, HL-60, Kasumi-1 and NB4 cell lines. And Dramatically induced cell apoptosis of FLT3-ITD, FLT3-ITD-expressing murine Ba/F3 and human OCI-AML3 cells. |
| Animal Protocol |
Animal/Disease Models: Female NSG mice with AML xenografts generated by intravenous (iv)injections of MOLM-13 cells[1]
Doses: 0.75 and 1.0 mg/kg Route of Administration: subcutaneous (sc)injection; 0.75 and 1.0 mg/kg one time/day 5 days a week until mice get moribund Experimental Results: Dramatically diminished the leukemia burden, circulating and BM leukemic human CD45+ cells. Dose-dependently prolonged the survival rate of mice. |
| References |
| Molecular Formula |
C29H31NO8
|
|---|---|
| Molecular Weight |
521.558348894119
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| Exact Mass |
521.204
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| CAS # |
1139253-73-8
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| PubChem CID |
49793307
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
829
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1C2=CC(OC)=CC(OC)=C2[C@]2(O)[C@H](O)[C@H](C(N(OC)C)=O)[C@@H](C3=CC=CC=C3)[C@]12C1=CC=C(OC)C=C1
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| InChi Key |
TZDAVNWDKGYBCW-IDAMAFBJSA-N
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| InChi Code |
InChI=1S/C29H31NO8/c1-30(37-5)27(32)23-24(17-9-7-6-8-10-17)29(18-11-13-19(34-2)14-12-18)28(33,26(23)31)25-21(36-4)15-20(35-3)16-22(25)38-29/h6-16,23-24,26,31,33H,1-5H3/t23-,24-,26-,28+,29+/m1/s1
|
| Chemical Name |
(1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-N,6,8-trimethoxy-3a-(4-methoxyphenyl)-N-methyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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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 : 200 mg/mL (383.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.59 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 50.0 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. Solubility in Formulation 2: ≥ 5 mg/mL (9.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9173 mL | 9.5866 mL | 19.1732 mL | |
| 5 mM | 0.3835 mL | 1.9173 mL | 3.8346 mL | |
| 10 mM | 0.1917 mL | 0.9587 mL | 1.9173 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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