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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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500mg |
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Purity: ≥98%
RPI-1 is an ATP-dependent RET kinase inhibitor. RPI-1, which is orally bioavailable, effectively treated 81% of treated tumors by causing growth arrest or regression. After treatment was halted, tumor inhibition remained (51%, P<0.05, 100 days) and 2/11 mice were cured. RPI-1 treatment of TT cells in vitro led to the in vivo effects of BAD activation, caspase cleavage, fragmentation of apoptotic DNA, and inhibition of VEGF production.
Targets |
JNK2; Akt
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ln Vitro |
Following 72 hours of treatment, RPI-1's growth-inhibitory effect on TPC-1 cells is susceptible, with an IC50 of 5.1 μM. In TPC-1 cells, RPI-1 (7.5–60 μM) prevents Ret/Ptc1 autophosphorylation. In TPC-1 cell culture conditions, RPI-1 inhibitory effects result in the inhibition of pathways involving JNK2 and AKT[1].
In NIH3T3 cells expressing the Ret mutant, the RPI-1 IC50 value is 3.6 µM compared to 16 µM in non-transfected NIH3T3 cells, and in RET mutant-transfected and H-RAS-transfected NIH3T3 cells, it was 2.4 µM and 26 µM, respectively, for colony formation in soft agar. After 24 hours of RPI-1 treatment, Ret protein and tyrosine phosphorylation in NIH3T3 cells expressing the Ret mutant were undetectable. RPI-1 inhibits TT cell proliferation, Ret tyrosine phosphorylation, Ret protein expression, and PLCgamma, ERKs, and AKT activation[2]. |
ln Vivo |
RPI-1 (50, 100 mg/kg; p.o.; twice a day for 10 days) inhibits TT xenograft tumor growth by 81%[2].
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Animal Protocol |
8- to 11-week-old female athymic nude CD-1 mice (bearing TT cells)[2]
50, 100 mg/kg P.o.; twice a day for 10 days |
References |
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Molecular Formula |
C17H15NO4
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Molecular Weight |
297.31
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Exact Mass |
297.1001
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Elemental Analysis |
C, 68.68; H, 5.09; N, 4.71; O, 21.53
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CAS # |
269730-03-2
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Related CAS # |
269730-03-2
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Appearance |
Solid powder
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SMILES |
COC1=C(C=C2C(=C1)/C(=C/C3=CC=C(C=C3)O)/C(=O)N2)OC
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InChi Key |
JGSMCYNBVCGIHC-QPEQYQDCSA-N
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InChi Code |
InChI=1S/C17H15NO4/c1-21-15-8-12-13(7-10-3-5-11(19)6-4-10)17(20)18-14(12)9-16(15)22-2/h3-9,19H,1-2H3,(H,18,20)/b13-7-
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Chemical Name |
(3Z)-3-[(4-hydroxyphenyl)methylidene]-5,6-dimethoxy-1H-indol-2-one
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Synonyms |
RPI1; RPI 1; RPI-1
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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: 59~125 mg/mL (198.5~420.4 mM)
Ethanol: ~2 mg/mL (~6.7 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (7.00 mM) in 10% DMSO + 90% (20% SBE-β-CD in 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 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3635 mL | 16.8175 mL | 33.6349 mL | |
5 mM | 0.6727 mL | 3.3635 mL | 6.7270 mL | |
10 mM | 0.3363 mL | 1.6817 mL | 3.3635 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.
Effects of RPI-1 on NIH3T3 MEN2A cells. A ) Ret autophosphorylation and expression. J Natl Cancer Inst . 2004 Jul 7;96(13):1006-14. td> |
Effect of RPI-1 on growth of TT cells. Cells were seeded in 96-well plates. J Natl Cancer Inst . 2004 Jul 7;96(13):1006-14. td> |
Effect of RPI-1 on Ret activation and signaling in human TT cells. J Natl Cancer Inst . 2004 Jul 7;96(13):1006-14. td> |
Effect of RPI-1 on human TT tumor xenograft growth. J Natl Cancer Inst . 2004 Jul 7;96(13):1006-14. td> |