| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
FHD-909 (LY4050784) (10 days) potently and selectively inhibited the proliferation of SMARCA4 mutant non-small cell lung cancer cell lines in vitro, with the median IC50 of SMARCA4 mutant cell lines being 33 times lower than that of SMARCA4 wild-type cell lines [1]. FHD-909 (0.1-100 nM) showed additive and synergistic antiproliferative activity against A549 SMARCA4 mutant non-small cell lung cancer cell lines in vitro when used in combination with cisplatin, paclitaxel, or pemetrexed [1]. FHD-909 (0.1-100 nM when used in combination with olomorasib; 0.1-100 nM when used in combination with LY4066434) showed synergistic antiproliferative activity against NCI-H2030 SMARCA4 mutant KRASG12C non-small cell lung cancer cell lines in vitro [1]. FHD-909 (concentrations of 0.1-1000 nM in PATU-8988T cells and 0.1-1000 nM in SNU-407 cells) showed synergistic antiproliferative activity against PATU-8988T pancreatic ductal adenocarcinoma cell line and SNU-407 colorectal cancer cell line in vitro [1]. When FHD-909 (concentrations of 1-10000 nM in A549 cells and 1-10000 nM in PATU-8988T cells) was used in combination with LY4066434, it showed synergistic antiproliferative activity against A549 non-small cell lung cancer cell line and PATU-8988T pancreatic ductal adenocarcinoma cell line in vitro [1]. FHD-909 effectively inhibited purified BRM ATPase with an IC50 value of 0.0025 μM, and its selectivity for BRM was 35.69 times higher than that for purified BRG1 ATPase [4].
|
|---|---|
| ln Vivo |
FHD-909 (LY4050784) (20-60 mg/kg; orally; twice daily; for 28 days) has shown potent and selective single-agent activity against SMARCA4G12C mutant non-small cell lung cancer (NSCLC) xenografts [1]. FHD-909 (60 mg/kg; orally; twice daily; for 28 days) enhances the antitumor activity of cisplatin and pemetrexed combined chemotherapy, resulting in tumor regression of SMARCA4G12C mutant NSCLC xenografts [1]. FHD-909 (40 mg/kg; orally; twice daily; for 28 days) enhances the antitumor activity of cisplatin and paclitaxel combined chemotherapy, resulting in tumor regression of SMARCA4G12C mutant NSCLC xenografts [1]. FHD-909 (20, 40 mg/kg; orally; twice daily; study days 22–49) enhanced the sensitivity of SMARCA4G12C mutant non-small cell lung cancer (NSCLC) xenografts to pembrolizumab and improved antitumor activity compared to monotherapy [1]. FHD-909 (40 mg/kg; orally; twice daily; 28 days) in combination with olomolasilub produced synergistic antitumor activity and sustained tumor regression in SMARCA4/KRASG12C comutated NSCLC xenografts [1]. FHD-909 (40 mg/kg; orally; twice daily; 28 days) in combination with LY4066434 produced synergistic antitumor activity and sustained tumor regression in SMARCA4/KRASG12S comutated NSCLC xenografts [1].
|
| References |
| Molecular Formula |
C29H25F2N5O5S
|
|---|---|
| Molecular Weight |
593.60
|
| CAS # |
3008577-34-9
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CC(F)=C(OCC[C@@H](S2(=O)=O)F)C2=C1)NCC3=CC4=C(C=N3)C=CC(N5C6=NC(C7CC7)=CC=C6OCC5)=N4
|
| Synonyms |
LY4050784
|
| 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 | 1.6846 mL | 8.4232 mL | 16.8464 mL | |
| 5 mM | 0.3369 mL | 1.6846 mL | 3.3693 mL | |
| 10 mM | 0.1685 mL | 0.8423 mL | 1.6846 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
