| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Ripretinib HCl (DCC2618; DCC-2618; Qinlock), the hydrochloride salt of DCC-2618, is an orally bioactive pan KIT and PDGFRA inhibitor approved in 2020 for the treatment of adults with advanced gastrointestinal stromal tumor. It functions by obstructing several additional kinase targets associated with systemic mastocytosis, including KIT D816V.
| ln Vitro |
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Enzyme Assay |
In order to assess KIT and BTK signaling, ROSAKIT WT, ROSAKIT D816V, HMC-1.1, and HMC-1.2 cells were incubated for 4 hours at 37°C in either control medium or DCC-2618 (0.5–5 μM). Western blotting was done essentially according to other instructions. In order to assess the downstream signaling pathways of KIT, HMC-1.1, HMC-1.2, ROSAKIT WT, and ROSAKIT D816V cells were initially pre-cultured for an entire night in Iscove-modified Dulbecco medium that was devoid of stem cell factor and fetal calf serum. DCC-2618 (0.001–10 μM) was then applied to 106 cells from each line for 90 minutes at 37°C. Following treatment, 10% stem cell factor-containing supernatants of Chinese hamster ovary cells transfected with the murine scf (kl) gene (CHO-KL) were added to ROSAKIT WT cells and incubated for 10 minutes at room temperature. After that, Western blotting was carried out essentially as previously mentioned.
|
||
| Cell Assay |
The survival and proliferation of drug-exposed cells—primary or cell line—were examined. In the Online Supplementary Methods, the bioassays used are described.
|
||
| Animal Protocol |
|
||
| References |
| Related CAS # |
1442472-39-0; 1225278-16-9
|
|---|---|
| Appearance |
Solid
|
| Synonyms |
DCC-2618 hydrochloride; DCC 2618 HCl; DCC2618; Ripretinibhydrochloride
|
| 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) |
|
|||
|---|---|---|---|---|
| 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.) |
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.
 DCC-2618 and its active metabolite DP-5439 inhibit proliferation of neoplastic mast cells.Haematologica.2018 May;103(5):799-809. |
|---|
 DCC-2618 inhibits phosphorylation of KIT and other targets in neoplastic mast cells.Haematologica.2018 May;103(5):799-809. |
Effects of DCC-2618 on anti-IgE-induced histamine release from normal basophils.Haematologica.2018 May;103(5):799-809. |
 DCC-2618 and DP-5439 induce apoptosis in neoplastic mast cells.Haematologica.2018 May;103(5):799-809. |
|---|
 Effects of DCC-2618 and DP-5439 on proliferation and survival of acute myeloid leukemia (AML) and chronic myelomonocytic leukemia (CMML).Haematologica.2018 May;103(5):799-809. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
