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| 25mg |
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| 50mg |
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Purity: ≥98%
Roblitinib (FGF-401) is a potent and highly selective inhibitor of human fibroblast growth factor receptor 4 (FGFR4) with an IC50 of 1.9 nM and with potential antineoplastic/anticancer activity. In tumor cells that overexpress FGFR4, FGF401 binds to the receptor and suppresses its activity, thereby preventing the growth of tumor cells. Tumor cell proliferation, differentiation, angiogenesis, and survival are all impacted by the receptor tyrosine kinase FGFR4, which is upregulated in some tumor cells. Currently undergoing phase I/II clinical studies, FGF401 is being developed for hepatocellular carcinoma. Oral FGF401 administration resulted in increased peripheral marker 7alpha-hydroxy-4-cholesten-3-one, induction of Cyp7a1, dog diarrhea, decreased serum cholesterol, and larger BA pools in preclinical studies involving mice and dogs. In the absence of any discernible negative histopathological findings in the liver or any other organ, FGF401 was also linked to increases in serum aminotransferases, particularly alanine aminotransferase (ALT).
| Targets |
FGFR4 (IC50 = 1.9 nM); FGFR1 (IC50 >10 μM); FGFR2 (IC50 >10 μM); FGFR3 (IC50 >10 μM); rat FGFR4 (IC50 >10 μM)
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| ln Vivo |
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| Enzyme Assay |
The regulation of bile acid (BA) homeostasis is significantly influenced by the FGF19-fibroblast growth factor receptor (FGFR4)-βKlotho (KLB) pathway. A subgroup of liver cancers, including hepatocellular carcinoma, have been shown to develop and progress due to aberrant activation of this pathway; as a result, FGFR4 has become a popular therapeutic target for these solid tumors.
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| Animal Protocol |
Male Wistar Hannover rats (Hep3B xenograft model)
10, 30, 100 mg/kg Gavage; for 10 days |
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| References | ||
| Additional Infomation |
Roblitinib is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, roblitinib binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival.
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| Molecular Formula |
C25H30N8O4
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|---|---|---|
| Molecular Weight |
506.57
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| Exact Mass |
506.239
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| Elemental Analysis |
C, 59.28; H, 5.97; N, 22.12; O, 12.63
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| CAS # |
1708971-55-4
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| Related CAS # |
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| PubChem CID |
118036971
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
852.1±65.0 °C at 760 mmHg
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| Flash Point |
469.1±34.3 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.654
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| LogP |
-0.15
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
37
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| Complexity |
865
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])N1C([H])([H])C1=C(C([H])=O)N=C2C(=C1[H])C([H])([H])C([H])([H])C([H])([H])N2C(N([H])C1C([H])=C(C(C#N)=C([H])N=1)N([H])C([H])([H])C([H])([H])OC([H])([H])[H])=O
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| InChi Key |
BHKDKKZMPODMIQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30N8O4/c1-31-7-8-32(23(35)15-31)14-18-10-17-4-3-6-33(24(17)29-21(18)16-34)25(36)30-22-11-20(27-5-9-37-2)19(12-26)13-28-22/h10-11,13,16H,3-9,14-15H2,1-2H3,(H2,27,28,30,36)
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| Chemical Name |
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9741 mL | 9.8703 mL | 19.7406 mL | |
| 5 mM | 0.3948 mL | 1.9741 mL | 3.9481 mL | |
| 10 mM | 0.1974 mL | 0.9870 mL | 1.9741 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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