| Size | Price | Stock | Qty |
|---|---|---|---|
| 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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| Other Sizes |
| Targets |
polycomb repressive complex 2; PRC2[1]
|
|---|---|
| ln Vivo |
ORIC-944 (30, 100, 200 mg/kg; oral; once daily for 50 days) induced significant tumor regression at all dose levels[3]. ORIC-944 (30 mg/kg; oral; once daily for 30 days) has potent single-agent activity against enzalutamide in a prostate cancer xenograft model [3].
|
| Animal Protocol |
Animal/Disease Models: KARPAS-422 DLBCL xenograft model[1]
Doses: 30, 100, 200 mg/kg Route of Administration: Oral gavage (p.o.) Experimental Results: Had well tolerated at all dose levels assessed compared to tazemetostat at a clinically relevant dose. Animal/Disease Models: 22Rv1 model Doses: 30 mg/kg Route of Administration: Oral gavage (p.o.) Experimental Results: Made average tumor volume ± SEM, with n=8-10/group. Had a significant difference in ORIC-944 treatment group vs vehicle. |
| References |
|
| Molecular Formula |
C26H25FN6O
|
|---|---|
| Molecular Weight |
456.51
|
| CAS # |
2369769-29-7
|
| Related CAS # |
ORIC-944 TFA
|
| PubChem CID |
155788096
|
| Appearance |
White to off-white solid powder
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| Density |
1.31±0.1 g/cm3(Predicted)
|
| LogP |
0
|
| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
744
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(NCC2=C3C(=CC=C2F)OCC3)=NC=C(C2=CC=C(CN(C)C)C=C2C)C2=NC(C#N)=CN12
|
| 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 : ~100 mg/mL (~219.05 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.48 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 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300, mix well; then add 50 μL Tween-80 to the above system, mix well; then continue to add 450 μL of normal saline to make up to 1 mL. Preparation of normal saline: Dissolve 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent normal saline solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.48 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 25.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1905 mL | 10.9527 mL | 21.9053 mL | |
| 5 mM | 0.4381 mL | 2.1905 mL | 4.3811 mL | |
| 10 mM | 0.2191 mL | 1.0953 mL | 2.1905 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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