| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of Paklatinib during lactation. The manufacturer recommends discontinuing breastfeeding during treatment and for two weeks after the last dose. The use of other medications is recommended, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. |
|---|---|
| References |
|
| Additional Infomation |
Parkinib citrate is the citrate form of parkinib. It is an antitumor drug and an EC 2.7.10.2 (non-specific protein tyrosine kinase) inhibitor. It contains parkinib (1+). Parkinib citrate is the citrate form of parkinib, an orally bioavailable inhibitor of Janus kinase 2 (JAK2), the JAK2 mutant JAK2V617F, and FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) with potential antitumor activity. After oral administration of parkinib citrate, parkinib competes with JAK2 and its mutant JAK2V617F for ATP binding sites, which may lead to inhibition of JAK2 activation, thereby inhibiting the JAK-STAT signaling pathway and inducing apoptosis. Furthermore, parkinib can also target FLT3, binding to and inhibiting its activity. This inhibits FLT3-mediated signaling and the proliferation of FLT3-expressing cancer cells. JAK2 is frequently upregulated or mutated in various cancer cells, playing a crucial role in tumor cell proliferation and survival. The JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity. FLT3 is a class III receptor tyrosine kinase (RTK) that is overexpressed or mutated in most B-cell lineage tumors and acute myeloid leukemia. Furthermore, JAK2 and FLT3 play key roles in inflammatory responses and the regulation of dendritic cell (DC) proliferation, differentiation, and function. Inhibition of JAK2 and FLT3-mediated signaling pathways may suppress DC generation and differentiation and may modulate inflammatory and immune responses.
See also: Paparkinib (containing the active ingredient). |
| Molecular Formula |
C34H40N4O10
|
|---|---|
| Molecular Weight |
664.70
|
| Exact Mass |
664.274
|
| CAS # |
1228923-42-9
|
| PubChem CID |
46216795
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
48
|
| Complexity |
871
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CN(CCOC2=CC=C3N=C4N=CC=C(C5=CC=CC(COCC=CCOCC2=C3)=C5)N4)CC1.OC(=O)CC(O)(C(=O)O)CC(=O)O |t:10,24|
|
| InChi Key |
BAHHBHSHSRTKNK-BJILWQEISA-N
|
| InChi Code |
InChI=1S/C28H32N4O3.C6H8O7/c1-2-13-32(12-1)14-17-35-27-9-8-25-19-24(27)21-34-16-4-3-15-33-20-22-6-5-7-23(18-22)26-10-11-29-28(30-25)31-26;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-11,18-19H,1-2,12-17,20-21H2,(H,29,30,31);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/b4-3+;
|
| Chemical Name |
2-hydroxypropane-1,2,3-tricarboxylic acid;(16E)-11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(24),2(27),3,5,8(26),9,11,16,21(25),22-decaene
|
| 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) |
Typically soluble in DMSO (e.g. 10 mM)
|
|---|---|
| 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 | 1.5044 mL | 7.5222 mL | 15.0444 mL | |
| 5 mM | 0.3009 mL | 1.5044 mL | 3.0089 mL | |
| 10 mM | 0.1504 mL | 0.7522 mL | 1.5044 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.
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