| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
RET (IC50 = 8 nM)
SPP-86 is a potent and selective inhibitor of RET tyrosine kinase, a receptor tyrosine kinase involved in cell proliferation, differentiation, and survival. By inhibiting RET kinase activity, it blocks RET-induced activation of the PI3K/Akt and MAPK signaling pathways. SPP-86 also inhibits RET-induced ERα phosphorylation in MCF7 cells. It is cell-permeable and exhibits additional inhibitory activity at EphA1, FGFR1, Flt4, Lck, and Yes. |
|---|---|
| ln Vitro |
SPP86 (0-10 μM)) inhibits MAPK signaling and proliferation in TPC1 cells expressing RET/PTC1, but not in 8505C or C643 cells[1].
SPP86 0-10 μM) prevents estrogen receptor (ER) phosphorylation and phosphatidylinositide 3-kinase (PI3K)/Akt and MAPK signaling from being induced by RET in MCF7 cells[1]. In vitro, SPP-86 inhibits RET tyrosine kinase with an IC50 of 8 nM. It inhibits RET-induced activation of the PI3K/Akt and MAPK signaling pathways in MCF7 cells. SPP-86 also inhibits RET-induced ERα phosphorylation. It inhibits proliferation of HCT 116 and TPC1 cells in vitro. Its in vitro activity is characterized by potent and selective RET inhibition and modulation of downstream signaling pathways. |
| ln Vivo |
In vivo, SPP-86 has been studied for its potential anti-cancer effects. As a RET inhibitor, it may block RET-driven tumor growth and proliferation. SPP-86 has potential for the treatment of cancers driven by RET mutations or overexpression. However, detailed in vivo efficacy data for specific disease models are limited. SPP-86 is primarily used as a research tool for studying RET biology.
|
| Enzyme Assay |
In vitro enzyme assays for SPP-86 typically involve measuring the inhibition of RET tyrosine kinase activity. The compound inhibits RET with an IC50 of 8 nM. Its selectivity over other kinases such as EphA1, FGFR1, Flt4, Lck, and Yes is also assessed. These assays confirm its mechanism of action as a RET tyrosine kinase inhibitor.
|
| Cell Assay |
In vitro cellular assays for SPP-86 typically involve treating cancer cell lines such as MCF7, HCT 116, and TPC1 with the compound and measuring cell proliferation, signaling pathway modulation, and ERα phosphorylation. SPP-86 inhibits RET-induced PI3K/Akt and MAPK signaling and RET-induced ERα phosphorylation in MCF7 cells. It inhibits proliferation of HCT 116 and TPC1 cells. These cell-based studies demonstrate its functional inhibition of RET signaling.
|
| Animal Protocol |
In vivo animal models for SPP-86 may include xenograft tumor models driven by RET mutations or overexpression. The compound is administered by appropriate routes, and tumor growth inhibition is measured. However, detailed animal protocol information is limited. SPP-86 is primarily used as a research tool for studying RET biology. SPP-86 has a molecular weight of 277.32 and a molecular formula of C16H15N5. Its CAS number is 1357349-91-7. The compound is a potent and selective cell-permeable inhibitor of RET tyrosine kinase. It is typically stored under appropriate conditions to maintain stability. SPP-86 is for research use only and not for human therapeutic use.
|
| Toxicity/Toxicokinetics |
SPP-86 is a RET tyrosine kinase inhibitor with a well-characterized mechanism of action. As with any kinase inhibitor, potential toxicity may include off-target effects on other kinases and disruption of normal cellular signaling. The compound's safety profile should be evaluated in preclinical toxicology studies. SPP-86 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying RET biology and cancer.
|
| References | |
| Additional Infomation |
SPP-86 (CAS# 1357349-91-7) is a potent and selective cell-permeable inhibitor of RET tyrosine kinase with an IC50 of 8 nM. It inhibits RET-induced PI3K/Akt and MAPK signaling and RET-induced ERα phosphorylation in MCF7 cells. SPP-86 inhibits proliferation of HCT 116 and TPC1 cells in vitro. The compound is for research use only and not for human therapeutic use.
|
| Molecular Formula |
C16H15N5
|
|---|---|
| Molecular Weight |
277.323802232742
|
| Exact Mass |
277.132
|
| Elemental Analysis |
C, 69.29; H, 5.45; N, 25.25
|
| CAS # |
1357349-91-7
|
| Related CAS # |
1357349-91-7
|
| PubChem CID |
66549796
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
2.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
417
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JQOIRTDBHMDWMT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H15N5/c1-11(2)21-16-14(15(17)18-10-19-16)13(20-21)9-8-12-6-4-3-5-7-12/h3-7,10-11H,1-2H3,(H2,17,18,19)
|
| Chemical Name |
3-(2-phenylethynyl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
|
| Synonyms |
SPP86; SPP 86; SPP-86
|
| 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) |
DMSO: 55~100 mg/mL (198.3~360.6 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6059 mL | 18.0297 mL | 36.0594 mL | |
| 5 mM | 0.7212 mL | 3.6059 mL | 7.2119 mL | |
| 10 mM | 0.3606 mL | 1.8030 mL | 3.6059 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
