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Cridanimod (XBIO-101; XBIO101; Virexxa) is a novel and potent immunomodulator and interferon inducer with antineoplastic activity. It acts as a progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod can increase progesterone receptor (PR) expression and is able to induce the expression of PR in endometrial cancer. This could increase the sensitivity of endometrial cancer cells to progestin monotherapy.
| ln Vivo |
The duration of cridanimod (intramuscular; 1-6 mg; twice weekly) was noticeably greater. IFNα and -β are markedly and dose-dependently increased in mice when treated with crinanimod [1].
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| Animal Protocol |
Animal/Disease Models: Athymic mice with hec50co cells [1]. 1]
Doses: 1, 3, 6 mg Route of Administration: IM; twice weekly Experimental Results: Dramatically prolonged survival. |
| References |
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| Additional Infomation |
Cridanimod is a member of acridines. It is functionally related to an acridone.
Cridanimod is a small molecule that can increase progesterone receptor (PR) expression, with potential antineoplastic adjuvant activity. Upon intramuscular administration, cridanimod is able to induce the expression of PR in endometrial cancer. This could increase the sensitivity of endometrial cancer cells to progestin monotherapy. In combination with a progestin, cancer cells could be eradicated through increased PR-mediated signaling, leading to an inhibition of luteinizing hormone (LH) release from the pituitary gland, via a negative feedback mechanism, and, eventually, an inhibition of estrogen release from the ovaries. This leads to an inhibition of cellular growth in estrogen-dependent tumor cells. In addition, this agent is able to increase the production and release of interferon (IFN) alpha and beta. PR is often downregulated in endometrial cancer and makes it resistant to progestin-mediated hormone therapy. |
| Molecular Formula |
C15H11NO3
|
|---|---|
| Molecular Weight |
253.257
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| Exact Mass |
253.073
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| CAS # |
38609-97-1
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| Related CAS # |
58880-43-6 (sodium);38609-97-1 (free acid);
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| PubChem CID |
38072
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
486.6±34.0 °C at 760 mmHg
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| Melting Point |
-289ºC (dec.)
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| Flash Point |
248.1±25.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.657
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| LogP |
2.03
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
356
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UOMKBIIXHQIERR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11NO3/c17-14(18)9-16-12-7-3-1-5-10(12)15(19)11-6-2-4-8-13(11)16/h1-8H,9H2,(H,17,18)
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| Chemical Name |
2-(9-oxoacridin-10(9H)-yl)acetic acid
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| Synonyms |
Cridanimod XBIO101 CycloferonXBIO-101 Virexxa Cyclopheron XBIO 101
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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 : ~125 mg/mL (~493.56 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (8.21 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 (8.21 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 20.8 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 | 3.9485 mL | 19.7426 mL | 39.4851 mL | |
| 5 mM | 0.7897 mL | 3.9485 mL | 7.8970 mL | |
| 10 mM | 0.3949 mL | 1.9743 mL | 3.9485 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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