Picropodophyllin
Based on 31 publication(s) in Google Scholar
Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.85%
- No. CAS: 477-47-4
- Fòrmula: C22H22O8
- Peso molecular:414.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Picropodophyllin
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
- Cancer Res. 2025 Feb 1;85(3):442-461. [Abstract]
- Transl Neurodegener. 2019 Mar 5:8:8. [Abstract]
- Nat Commun. 2025 Feb 25;16(1):1774. [Abstract]
- Nat Commun. 2023 Sep 30;14(1):6117. [Abstract]
- Adv Sci (Weinh). 2025 Jul 18:e01341. [Abstract]
- Adv Sci (Weinh). 2024 Feb;11(6):e2305913. [Abstract]
- Cell Death Dis. 2022 Aug 5;13(8):682. [Abstract]
- Environ Sci Technol. 2020 Sep 1;54(17):10783-10796. [Abstract]
- Phytomedicine. 2026 Apr:153:157996. [Abstract]
- Phytomedicine. 2021 May:85:153541. [Abstract]
- Cell Death Discov. 2021 Sep 18;7(1):251. [Abstract]
- Acta Pharmacol Sin. 2016 Feb;37(2):217-27. [Abstract]
- EMBO J. 2019 Aug 1;38(15):e101964. [Abstract]
- Phytother Res. 2023 Oct;37(10):4740-4754. [Abstract]
- Clin Transl Med. 2024 Jun;14(6):e1725. [Abstract]
- J Agric Food Chem. 2022 Mar 2;70(8):2752-2761. [Abstract]
- Ecotoxicol Environ Saf. 2024 Sep 15:283:116804. [Abstract]
- Eur J Pharmacol. 2026 Feb 28:1016:178651. [Abstract]
- Int Immunopharmacol. 2026 Mar 15:173:116323. [Abstract]
- Mol Med Rep. 2021 Feb;23(2):138. [Abstract]
- Sci Rep. 2026 Jan 27;16(1):6312. [Abstract]
- Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]
- Adv Biol (Weinh). 2025 Jul 18:e00730. [Abstract]
- Exp Eye Res. 2025 Jan:250:110158. [Abstract]
- SSRN. 2026 Apr 21.
- bioRxiv. 2025 February 27.
- Research Square Preprint. 2024 Dec 17.
- Research Square Preprint. 2023 Nov 21.
- Research Square Print. 2023 Feb 7.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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WB
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WB
Actividad biológica
IC50: 1 nM (IGF-1R)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
6 μM
Compound: 2
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Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
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[PMID: 7673931] |
| A549 | IC50 |
60 nM
Compound: 2b
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In vitro cytotoxicity against the A-549 (human lung carcinoma) neoplastic cell line
In vitro cytotoxicity against the A-549 (human lung carcinoma) neoplastic cell line
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[PMID: 14980682] |
| HT-29 | IC50 |
6 μM
Compound: 2
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Cytotoxicity against human HT-29 cells
Cytotoxicity against human HT-29 cells
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[PMID: 7673931] |
| HT-29 | IC50 |
60 nM
Compound: 2b
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In vitro cytotoxicity against the HT-29 (human colon carcinoma) neoplastic cell line
In vitro cytotoxicity against the HT-29 (human colon carcinoma) neoplastic cell line
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[PMID: 14980682] |
| P388 | IC50 |
6 μM
Compound: 2
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Cytotoxicity against mouse P388 cells
Cytotoxicity against mouse P388 cells
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[PMID: 7673931] |
| P388 | IC50 |
60 nM
Compound: 2b
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In vitro cytotoxicity against the P-388 (from DBA/2 mouse) neoplastic cell line
In vitro cytotoxicity against the P-388 (from DBA/2 mouse) neoplastic cell line
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[PMID: 14980682] |
Picropodophyllin (AXL1717) (0.5, 2.5, 10 μM) potently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation in intact cells. Picropodophyllin (AXL1717) also inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells[1].Picropodophyllin (AXL1717) synergistically sensitizes HMCL, primary human MM and murine 5T33MM cells to ABT-737 and ABT-199 via further decreasing cell viability and enhancing apoptosis[3]. Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 477-47-4
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Appearance Solid
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Peso molecular 414.41
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Fòrmula C22H22O8
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Color White to off-white
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SMILES
O=C1OC[C@]2([H])[C@@H](O)C3=C(C=C4OCOC4=C3)[C@@H](C5=CC(OC)=C(OC)C(OC)=C5)[C@@]21[H]
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Synonyms
AXL1717; Picropodophyllotoxin; PPP
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (31)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Nat Nanotechnol
Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]2021 Jul;16(7):830-839. PMID: 33958764
Picropodophyllin purchased from MedChemExpress. Usage Cited in: Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
Animals bearing subcutaneous (s.c.) iKras tumors were treated with AXL1717 (Picropodophyllin; 15 mg/kg dissolved in 100 μL mixture of 10% DMSO and 90% olive oil, via i.p. injection for 8 hr, 1 day, or 4 days prior to nanoparticle injection (1, 2 , or 5 days prior to tissue harvesting)), and biodistribution was measured 24 hr later by fluorescent reflectance imaging.
Picropodophyllin purchased from MedChemExpress. Usage Cited in: Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
Mice bearing subcutaneous iKras tumors were treated with vehicle controls, nab-PTX, AXL1717 (Picropodophyllin; 15 mg/kg dissolved in 100 μL mixture of 10% DMSO and 90% olive oil, via i.p. injection for 8 hr, 1 day, or 4 days prior to nanoparticle injection (1, 2 , or 5 days prior to tissue harvesting)), simultaneous treatment of both (Co-tx), or sequential treatment of both (Sep-tx) with equal cumulative doses. Tumor volume and survival based on humane endpoint (f, n=4 per group, log-rank test) were monitored.
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Cancer Res
Mutant PP2A Induces IGFBP2 Secretion to Promote Development of High-Grade Uterine Cancer. [Abstract]2025 Feb 1;85(3):442-461. PMID: 39531506 -
Transl Neurodegener
Enriched gestation activates the IGF pathway to evoke embryo-adult benefits to prevent Alzheimer's disease. [Abstract]2019 Mar 5:8:8. PMID: 30867903 -
Nat Commun
Attenuated growth factor signaling during cell death initiation sensitizes membranes towards peroxidation. [Abstract]2025 Feb 25;16(1):1774. PMID: 40000627
Picropodophyllin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 25;16(1):1774. [Abstract]
Viable cell numbers and PUFA-PC ratio after treatment with LY294002 (iPI3K, 10 µM), picropodophyllin (iRTK, 10 µM), ipatasertib (iAkt, 10 µM), or fatostatin (iSREBP1, 20 µM) for 48 h.
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Nat Commun
IGF1R-phosphorylated PYCR1 facilitates ELK4 transcriptional activity and sustains tumor growth under hypoxia. [Abstract]2023 Sep 30;14(1):6117. PMID: 37777542 -
Adv Sci (Weinh)
Targeting IGF1R Overcomes Armored and Cold Tumor Microenvironment and Boosts Immune Checkpoint Blockade in Triple-Negative Breast Cancer. [Abstract]2025 Jul 18:e01341. PMID: 40679093 -
Adv Sci (Weinh)
2024 Feb;11(6):e2305913. PMID: 38059822 -
Cell Death Dis
Gemcitabine resistance of pancreatic cancer cells is mediated by IGF1R dependent upregulation of CD44 expression and isoform switching. [Abstract]2022 Aug 5;13(8):682. PMID: 35931675 -
Environ Sci Technol
Tris(1,3-dichloro-2-propyl)phosphate Reduces the Lifespan via Activation of an Unconventional Insulin/Insulin-Like Growth Factor-1 Signaling Pathway. [Abstract]2020 Sep 1;54(17):10783-10796. PMID: 32786597 -
Phytomedicine
Pyrroloquinoline quinone alleviates age-related osteoarthritis via nuclear factor erythroid 2-related factor 2-mediated stress response and insulin-like growth factor 1 receptor upregulation. [Abstract]2026 Apr:153:157996. PMID: 41763140 -
Phytomedicine
Gypenoside XLIX protects against acute kidney injury by suppressing IGFBP7/IGF1R-mediated programmed cell death and inflammation. [Abstract]2021 May:85:153541. PMID: 33773190 -
Cell Death Discov
Trimetazidine attenuates dexamethasone-induced muscle atrophy via inhibiting NLRP3/GSDMD pathway-mediated pyroptosis. [Abstract]2021 Sep 18;7(1):251. PMID: 34537816 -
Acta Pharmacol Sin
Insulin deficiency induces rat renal mesangial cell dysfunction via activation of IGF-1/IGF-1R pathway. [Abstract]2016 Feb;37(2):217-27. PMID: 26775660
Picropodophyllin purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2016 Feb;37(2):217-27. [Abstract]
The phosphorylation of IGF-1R is observed by a Western blot assay after the cells are pretreated with PPP 50 nM or a diluent for 60 min and deprived of insulin for 5 min.
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EMBO J
GSTZ1-1 Deficiency Activates NRF2/IGF1R Axis in HCC via Accumulation of Oncometabolite Succinylacetone. [Abstract]2019 Aug 1;38(15):e101964. PMID: 31267557 -
Phytother Res
Targeting HSP90 with picropodophyllin suppresses gastric cancer tumorigenesis by disrupting the association of HSP90 and AKT. [Abstract]2023 Oct;37(10):4740-4754. PMID: 37559472 -
Clin Transl Med
Deletion of endothelial IGFBP5 protects against ischaemic hindlimb injury by promoting angiogenesis. [Abstract]2024 Jun;14(6):e1725. PMID: 38886900 -
J Agric Food Chem
Dietary Inhibitors of CYP3A4 Are Revealed Using Virtual Screening by Using a New Deep-Learning Classifier. [Abstract]2022 Mar 2;70(8):2752-2761. PMID: 35104412 -
Ecotoxicol Environ Saf
Neohesperidin alleviates the inhibitory effect of bisphenol A on the myogenic differentiation of umbilical cord mesenchymal stem cells via the IGF1R/AKT1/RHOA signaling pathway. [Abstract]2024 Sep 15:283:116804. PMID: 39083871 -
Eur J Pharmacol
Isoliensinine ameliorates postoperative neurocognitive disorder in aged mice by restoring hippocampal IGF-1 receptor signaling and suppressing oxidative stress and neuroinflammation. [Abstract]2026 Feb 28:1016:178651. PMID: 41655685 -
Int Immunopharmacol
IGF-1 ameliorates the blood brain barrier disruption induced by the neonatal hypoxia-ischemia. [Abstract]2026 Mar 15:173:116323. PMID: 41655435 -
Mol Med Rep
Inhibition of SNCG suppresses the proliferation of lung cancer cells induced by high glucose. [Abstract]2021 Feb;23(2):138. PMID: 33313952 -
Sci Rep
Therapeutic effects of IGF-2 on NMOSD by inhibiting astrocyte apoptosis through modulation of the IGF-1R/PI3K/AKT signaling pathway. [Abstract]2026 Jan 27;16(1):6312. PMID: 41593135 -
Cancer Sci
2018 Apr;109(4):1166-1176. PMID: 29465762
Picropodophyllin purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]
PPP downregulates IGF-1R as well as the total and phosphor-HER2 levels in the MKN7 cell line.
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Adv Biol (Weinh)
2025 Jul 18:e00730. PMID: 40679030 -
Exp Eye Res
SN promote retinal pathological neovascularization through activation of EGFR, IR and IGF-1R. [Abstract]2025 Jan:250:110158. PMID: 39549871 -
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Solvente y solubilidad
DMSO : 50 mg/mL (120.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 3 mg/mL (7.24 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 2 mg/mL (4.83 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Four to 5-week-old pathogen-free SCID mice are used and housed within plastic isolators in a sterile facility. ES-1, BE, and PC3 cells (all proved to express IGF-1R), or R-v-src (IGF-1R negative) and P12 (overexpressing IGF-1 and IGF-1R), are injected s.c. at 107 cells/mice in a 0.2 mL volume of sterile saline solution. Immunocompetent Balb-c mice are injected with 107JC murine breast cancer cells per mouse in 0.15 mL volume of sterile saline solution. Experimental treatments with Picropodophyllin (AXL1717) (20 mg/kg/12 h) are performed by daily i.p. injections of the compound in 10 μL volume of DMSO: vegetable oil, 10:1 (v/v). Control mice are treated with the vehicle only. Three animals are treated in each group. Tumor growth is measured every second day using vernier calipers, and the tumor volumes are calculated. The mice are carefully observed for the presence of side effects and are sacrificed at the end of the experiments for histological analysis of the lesions. A separate experiment on Picropodophyllin (AXL1717)-treated (systemically and locally) tumor-free mice, including histological analyses of various organs, confirms previous observations that Picropodophyllin (AXL1717) appears to be nontoxic.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (288 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Girnita A, et al. Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth. Cancer Res. 2004 Jan 1;64(1):236-42. [Content Brief]
[2]. Menu E, et al. Inhibiting the IGF-1 receptor tyrosine kinase with the cyclolignan PPP: an in vitro and in vivo study in the 5T33MM mouse model. Blood. 2006 Jan 15;107(2):655-60. Epub 2005 Jul 26. [Content Brief]
[3]. Bieghs L, et al. The IGF-1 receptor inhibitor picropodophyllin potentiates the anti-myeloma activity of a BH3-mimetic. Oncotarget. 2014 Nov 30;5(22):11193-208. [Content Brief]
[4]. Tomizawa M, et al. Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells. Oncol Lett. 2014 Nov;8(5):2023-2026. Epub 2014 Aug 27. [Content Brief]
[5]. Stromberg T, et al. IGF-1 receptor tyrosine kinase inhibition by the cyclolignan PPP induces G2/M-phase accumulation and apoptosis in multiple myeloma cells. Blood. 2006 Jan 15;107(2):669-78. Epub 2005 Sep 15. [Content Brief]
[6]. Kong YL, et al. Insulin deficiency induces rat renal mesangial cell dysfunction via activation of IGF-1/IGF-1R pathway. Acta Pharmacol Sin. 2016 Feb;37(2):217-27. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4131 mL | 12.0653 mL | 24.1307 mL | 60.3267 mL |
| 5 mM | 0.4826 mL | 2.4131 mL | 4.8261 mL | 12.0653 mL | |
| 10 mM | 0.2413 mL | 1.2065 mL | 2.4131 mL | 6.0327 mL | |
| 15 mM | 0.1609 mL | 0.8044 mL | 1.6087 mL | 4.0218 mL | |
| 20 mM | 0.1207 mL | 0.6033 mL | 1.2065 mL | 3.0163 mL | |
| 25 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4131 mL | |
| 30 mM | 0.0804 mL | 0.4022 mL | 0.8044 mL | 2.0109 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6033 mL | 1.5082 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4022 mL | 1.0054 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7541 mL | |
| 100 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |
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