| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| References | |
|---|---|
| Additional Infomation |
Casdatifan is a small molecule drug. The International Nonproprietary Name (INN) prefix "-tifan" in its name indicates that casdatifan is a hypoxia-inducible factor (HIF)-2α inhibitor. Casdatifan is currently being investigated in the clinical trial NCT07000149 (a study investigating the efficacy and safety of Volrustomig±casdatifan versus nivolumab + ipilimumab as a first-line treatment for advanced clear cell renal cell carcinoma). The monoisotope molecular weight of casdatifan is 439.09 Da. Casdatifan is an orally bioavailable allosteric inhibitor of hypoxia-inducible factor (HIF)-2α with potential antitumor activity. After oral administration, casdatifan targets and allosterically binds to the hydrophobic pocket on HIF-2α, leading to a conformational change that prevents HIF-2α from forming a heterodimer with HIF-1β and inhibits its binding to hypoxia-responsive element (HRE) binding sites on DNA. This leads to reduced transcription and expression of downstream target genes of HIF-2α, many of which regulate tumor cell growth and survival. Blocking HIF-2α reduces the proliferation of HIF-2α-expressing tumor cells. HIF-2α is a heterodimeric transcription factor that is overexpressed under hypoxic conditions in various cancer cell types, promoting tumor proliferation, progression, and metastasis.
|
| Molecular Formula |
C21H17F4NO3S
|
|---|---|
| Molecular Weight |
439.42
|
| Exact Mass |
439.087
|
| CAS # |
2709069-30-5
|
| PubChem CID |
156859185
|
| Appearance |
White to off-white solid
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
30
|
| Complexity |
811
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
CS(=O)(=O)C1=C2[C@@H]([C@@H](CC2=C(C=C1)[C@H]3C[C@@H]([C@@H](C4=CC(=CC(=C34)C#N)F)F)F)F)O
|
| InChi Key |
KHBHHNNBNHHGPE-QCCZFBHPSA-N
|
| InChi Code |
InChI=1S/C21H17F4NO3S/c1-30(28,29)17-3-2-11(13-7-16(24)21(27)19(13)17)12-6-15(23)20(25)14-5-10(22)4-9(8-26)18(12)14/h2-5,12,15-16,20-21,27H,6-7H2,1H3/t12-,15+,16-,20-,21-/m1/s1
|
| Chemical Name |
(5R,6S,8R)-3,5,6-trifluoro-8-[(1S,2R)-2-fluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl]-5,6,7,8-tetrahydronaphthalene-1-carbonitrile
|
| Synonyms |
AB521
|
| HS Tariff Code |
2934.99.9001
|
| 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 (~227.6 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.69 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 2.5 mg/mL (5.69 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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 3: ≥ 2.5 mg/mL (5.69 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 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 | 2.2757 mL | 11.3786 mL | 22.7573 mL | |
| 5 mM | 0.4551 mL | 2.2757 mL | 4.5515 mL | |
| 10 mM | 0.2276 mL | 1.1379 mL | 2.2757 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.
Link: https://clinicaltrials.gov/ct2/show/NCT07011719
Conditions:Metastatic Clear Cell Renal Cell Carcinoma|Advanced Clear Cell Renal Cell CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT05536141
Conditions:Clear Cell Renal Cell Carcinoma|Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT07397611
Conditions:Renal Cell Carcinoma|Kidney Cancer|Kidney Neoplasm|Renal Carcinoma
Title:A Study to Investigate the Efficacy and Safety of Volrustomig ± Casdatifan vs Nivolumab + Ipilimumab as 1L Treatment for Advanced ccRCC
Status:Active, not recruiting
updateDate:2026-03-10
Ctid:NCT07000149
Link: https://clinicaltrials.gov/ct2/show/NCT07000149
Conditions:Advanced Clear Cell Renal Cell CarcinomaLink: https://clinicaltrials.gov/ct2/show/NCT06919991
Conditions:Healthy ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT06191796
Conditions:Advanced Clear Cell Renal Cell Carcinoma or Other Advanced Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT05117554
Conditions:Healthy ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT05999513
Conditions:Healthy ParticipantsProducts are for research use only; We do not sell to patients
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