Pacritinib (SB1518) (Synonyms: SB1518) |
| رقم الكتالوجGC14676 |
Pacritinib (SB1518) (SB1518) هو مثبط قوي لكل من النوع البري JAK2 (IC50 = 23 نانومتر) و JAK2V617F متحولة (IC50 = 19 نانومتر). يثبط Pacritinib (SB1518) أيضًا FLT3 (IC50 = 22 نانومتر) و FLT3D835Y المتحولة (IC50 = 6 نانومتر).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 937272-79-2
Sample solution is provided at 25 µL, 10mM.
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Pacritinib is a small molecule inhibitor of Janus kinase 2/Fms-like tyrosine kinase-3 (JAK2/FLT3) with IC50 values of 23nM, 19nM and 22nM, respectively for JAK2WT, JAK2V617F and FLT3 [1].
Pacritinib inhibits the JAK2-mediated production of p-STAT5 and p-STAT3 in Ba/F3 cells and the production of p-FLT3 and p-STAT5 in MV4-11 cells. It is less active against CYP3A4 and has good selectivity and microsomal stability. Pacritinib is proved to be high permeable in a Caco-2 bidirectional permeability assay. Additionally, pacritinib has a good oral bioavailability. In the Ba/F3-JAK2V617F mouse allograft, 150mg/kg treatment of pacritinib significantly alleviates the disease symptoms. In the MV4-11 xenografts, 50mg/kg and 100 mg/kg pacritinib treatments both show a significantly increased median survival of 55 days [1].
References:
[1] William AD, Lee AC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Tan E, Chen D, Williams M, Sun ET, Goh KC, Ong WC, Goh SK, Hart S, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW. Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma. J Med Chem. 2011 Jul 14;54(13):4638-58.
| Cas No. | 937272-79-2 | SDF | |
| المرادفات | SB1518 | ||
| Chemical Name | AN2728;AN 2728 | ||
| Canonical SMILES | [H]C1([H])N(C([H])([H])C([H])([H])OC(C([H])=C2[H])=C(C([H])([H])OC([H])([H])/C([H])=C([H])\C([H])([H])OC([H])([H])C3=C([H])C4=C([H])C([H])=C3[H])C([H])=C2N([H])C5=NC([H])=C([H])C4=N5)C([H])([H])C([H])([H])C1([H])[H] | ||
| Formula | C28H32N4O3 | M.Wt | 472.58 |
| الذوبان | ≥ 11.05mg/mL in DMSO with gentle warming | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.116 mL | 10.5802 mL | 21.1604 mL |
| 5 mM | 0.4232 mL | 2.116 mL | 4.2321 mL |
| 10 mM | 0.2116 mL | 1.058 mL | 2.116 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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