| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
| Targets |
CFLZ-171 TFA salt itself does not have a direct pharmacological target as it is a synthetic intermediate rather than an active pharmaceutical ingredient. However, it is used in the synthesis of carfilzomib, which targets the 20S proteasome, specifically the chymotrypsin-like activity of the proteasome. Carfilzomib irreversibly binds to the N-terminal threonine of the proteasome's active site, inhibiting protein degradation and leading to apoptosis in cancer cells.
|
|---|---|
| ln Vitro |
As a synthetic intermediate, CFLZ-171 TFA salt does not have intrinsic in vitro biological activity. Its role is strictly as a chemical precursor in the multi-step synthesis of carfilzomib. The compound is used in organic synthesis reactions to construct the complex molecular architecture of the proteasome inhibitor. Its chemical properties, including reactivity and stability, are characterized for synthetic chemistry applications rather than biological assays.
|
| ln Vivo |
CFLZ-171 TFA salt is not a therapeutic agent and does not have in vivo biological activity. Its significance lies in its use as a key intermediate for manufacturing carfilzomib, which is clinically used for the treatment of multiple myeloma. The in vivo efficacy of carfilzomib, the final drug product, has been demonstrated in clinical trials showing significant antitumor activity in patients with relapsed and refractory multiple myeloma.
|
| Enzyme Assay |
CFLZ-171 TFA salt is used in chemical synthesis protocols for the preparation of carfilzomib. The compound is typically handled in organic solvents such as DMSO. Reaction conditions are optimized for the epoxide opening and peptide coupling steps. The progress of reactions is monitored by TLC or HPLC, and the intermediate is purified by column chromatography. Characterization is performed using NMR and mass spectrometry to confirm structure and purity.
|
| Cell Assay |
Cellular assays are not performed with CFLZ-171 TFA salt as it is a synthetic intermediate. The compound is used exclusively in chemical synthesis laboratories for the preparation of carfilzomib. For biological evaluation, the final drug product carfilzomib is tested in cancer cell lines to assess proteasome inhibition and cytotoxicity. Cell-based assays for carfilzomib include measuring proteasome activity, apoptosis induction, and cell viability in multiple myeloma cell lines.
|
| Animal Protocol |
Animal studies are not conducted with CFLZ-171 TFA salt itself. The compound is used in the chemical synthesis of carfilzomib, which is then evaluated in animal models of cancer. Carfilzomib has been studied in murine xenograft models of multiple myeloma, showing significant tumor growth inhibition. Pharmacokinetic and toxicological studies of carfilzomib have been conducted in various animal species to support clinical development.
|
| ADME/Pharmacokinetics |
CFLZ-171 TFA salt has a molecular formula of C₁₁H₁₈F₃NO₄, molecular weight of 285.26, and CAS number 247068-85-5. It has a LogP of 2.051 and two hydrogen bond donors. The compound typically exists as a solid at room temperature. For storage, powder should be kept at -20°C for up to 3 years, and in solvent at -80°C for 6 months or -20°C for 1 month. It is stable at ambient temperature for several days during shipping.
|
| Toxicity/Toxicokinetics |
CFLZ-171 TFA salt is a chemical intermediate and should be handled with appropriate laboratory safety precautions. As with most organic compounds, it may cause skin and eye irritation upon contact. Toxicity data are limited as the compound is not intended for human consumption. Standard personal protective equipment including gloves, lab coat, and safety goggles should be worn when handling. The compound is for research use only and not for human therapeutic applications.
|
| Additional Infomation |
CFLZ-171 TFA salt (PR171 intermediate) is a crucial synthetic building block for carfilzomib (Kyprolis), a second-generation proteasome inhibitor approved by the FDA in 2012 for the treatment of relapsed and refractory multiple myeloma. Carfilzomib is a tetrapeptide epoxyketone that irreversibly inhibits the proteasome and has shown superior efficacy compared to bortezomib in clinical studies. The intermediate is commercially available for research and pharmaceutical manufacturing purposes. It is exclusively used for scientific research and not for patient use.
|
| Molecular Formula |
C11H18F3NO4
|
|---|---|
| Molecular Weight |
285.2601
|
| Exact Mass |
285.118
|
| CAS # |
247068-85-5
|
| PubChem CID |
78358372
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
2.051
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
19
|
| Complexity |
274
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
FC(C(=O)O[H])(F)F.O1C([H])([H])[C@]1(C([H])([H])[H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])[H])=O
|
| InChi Key |
OWGGQBZQMQMPBI-DKXTVVGFSA-N
|
| InChi Code |
InChI=1S/C9H17NO2.C2HF3O2/c1-6(2)4-7(10)8(11)9(3)5-12-9;3-2(4,5)1(6)7/h6-7H,4-5,10H2,1-3H3;(H,6,7)/t7-,9+;/m0./s1
|
| Chemical Name |
(2S)-2-amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]pentan-1-one;2,2,2-trifluoroacetic acid
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 3.5056 mL | 17.5279 mL | 35.0557 mL | |
| 5 mM | 0.7011 mL | 3.5056 mL | 7.0111 mL | |
| 10 mM | 0.3506 mL | 1.7528 mL | 3.5056 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
