Abemaciclib methanesulfonate
Based on 125 publication(s) in Google Scholar
Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective and BBB-permeable CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.84%
- CAS No.: 1231930-82-7
- Formule: C28H36F2N8O3S
- Masse moléculaire:602.70
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Abemaciclib methanesulfonate
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Nature. 2017 Aug 24;548(7668):471-475. [Abstract]
- Cancer Cell. 2024 Aug 27:S1535-6108(24)00305-2. [Abstract]
- Cell. 2025 Oct 30;188(22):6301-6316.e29. [Abstract]
- Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
- Cell. 2018 Nov 1;175(4):984-997.e24. [Abstract]
- Cancer Discov. 2024 Mar 1;14(3):446-467. [Abstract]
- Nat Cancer. 2021 Apr;2(4):429-443. [Abstract]
- Nat Metab. 2020 Jan;2(1):41-49. [Abstract]
- Bioact Mater. 2021 Sep 8:10:247-254. [Abstract]
- Adv Funct Mater. 2021 Apr 30.
- Mol Cell. 2025 Sep 4;85(17):3333-3342.e4. [Abstract]
- Cancer Res. 2023 Oct 2;83(19):3264-3283. [Abstract]
- Cancer Res. 2022 May 16;82(10):1890-1908. [Abstract]
- Cancer Res. 2019 Oct 15;79(20):5245-5259. [Abstract]
- Mol Cell. 2017 Oct 19;68(2):336-349.e6. [Abstract]
- Cancer Res. 2017 May 1;77(9):2488-2499. [Abstract]
- Cancer Res. 2016 Nov 15;76(22):6723-6734. [Abstract]
- Nat Commun. 2026 Jan 22;17(1):619. [Abstract]
- Nat Commun. 2025 Jan 9;16(1):541. [Abstract]
- Nat Commun. 2022 Aug 10;13(1):4689. [Abstract]
- Nat Commun. 2021 Nov 16;12(1):6607. [Abstract]
- Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]
- Nat Commun. 2019 Jun 28;10(1):2860. [Abstract]
- Nat Commun. 2017 Jun 27;8:15916. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2026 Mar;13(14):e13135. [Abstract]
- Adv Sci (Weinh). 2022 Aug 2;e2201834. [Abstract]
- Adv Sci (Weinh). 2020 Aug 4;7(18):2000906. [Abstract]
- J Exp Clin Cancer Res. 2022 Apr 21;41(1):149. [Abstract]
- J Nanobiotechnology. 2025 Jan 3;23(1):3. [Abstract]
- Sci Adv. 2026 Jun 12;12(24):eaef1962. [Abstract]
- J Biomed Sci. 2025 Aug 20;32(1):79. [Abstract]
- Blood Cancer J. 2022 Jan 11;12(1):5. [Abstract]
- Cell Rep Med. 2025 Dec 29:102526. [Abstract]
- Clin Cancer Res. 2024 May 8. [Abstract]
- Int J Biol Sci. 2019 Jan 1;15(3):522-532. [Abstract]
- Cell Death Dis. 2020 Oct 28;11(10):925. [Abstract]
- Cell Death Dis. 2019 Mar 20;10(4):271. [Abstract]
- J Pharm Anal. 2025 Jan;15(1):101068. [Abstract]
- Int J Biol Macromol. 2025 Dec 9;337(Pt 2):149613. [Abstract]
- Phytomedicine. 2026 May:154:158042. [Abstract]
- EMBO Mol Med. 2025 Aug 29. [Abstract]
- EMBO J. 2024 Dec;43(23):5972-6000. [Abstract]
- EMBO J. 2024 Oct;43(19):4406-4436. [Abstract]
- EMBO J. 2022 Mar 15;41(6):e108946. [Abstract]
- Free Radic Biol Med. 2026 Aug 16:252:493-508.
- ACS Appl Mater Interfaces. 2022 May 11;14(18):20628-20640. [Abstract]
- NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]
- NPJ Precis Oncol. 2021 Mar 19;5(1):20. [Abstract]
- NPJ Breast Cancer. 2026 Feb 12. [Abstract]
- NPJ Breast Cancer. 2025 Dec 3;11(1):135. [Abstract]
- Biomed Pharmacother. 2025 Aug:189:118340. [Abstract]
- Cell Chem Biol. 2019 Aug 15;26(8):1067-1080.e8. [Abstract]
- Cell Rep. 2024 Dec 30;44(1):115116. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Cell Rep. 2022 Dec 20;41(12):111826. [Abstract]
- Cell Rep. 2022 Sep 13;40(11):111331. [Abstract]
- Cell Rep. 2017 Oct 31;21(5):1386-1398. [Abstract]
- Clin Transl Med. 2026 May;16(5):e70669.
- J Med Chem. 2023 Mar 23;66(6):4106-4130. [Abstract]
- Br J Cancer. 2022 Jun;126(11):1616-1626. [Abstract]
- JCI Insight. 2022 Feb 8;7(3):e154402. [Abstract]
- Int J Mol Med. 2025 Nov;56(5):167. [Abstract]
- Acta Neuropathol Commun. 2025 Jun 28;13(1):143. [Abstract]
- Breast Cancer Res. 2019 Dec 26;21(1):150. [Abstract]
- Biochem Pharmacol. 2017 Jan 15:124:29-42. [Abstract]
- Mol Cancer Ther. 2025 Jul 2. [Abstract]
- Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]
- Commun Biol. 2021 Mar 25;4(1):399. [Abstract]
- Cancer Gene Ther. 2025 Aug 14. [Abstract]
- Int J Mol Sci. 2022 Feb 24;23(5):2493. [Abstract]
- Int J Mol Sci. 2021 Jan 8;22(2):575. [Abstract]
- Pharmaceuticals (Basel). 2026 May 19;19(5):795. [Abstract]
- Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]
- Transl Oncol. 2025 Jan 3:52:102264. [Abstract]
- J Biol Chem. 2025 Jan 16:108196. [Abstract]
- Sci Rep. 2024 May 8;14(1):10582. [Abstract]
- Sci Rep. 2022 Jul 20;12(1):12420. [Abstract]
- Sci Rep. 2019 Oct 22;9(1):15099. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363. [Abstract]
- Heliyon. 2023 Sep 14;9(9):e19760. [Abstract]
- Transl Lung Cancer Res. 2024 May 31;13(5):1032-1046. [Abstract]
- Front Oncol. 2021 Jul 13:11:704042. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2023 Jul;396(7):1435-1450. [Abstract]
- Nutrition. 2019 Apr:60:217-226. [Abstract]
- R Soc Open Sci. 2019 Jan 23;6(1):181714. [Abstract]
- J Cell Biochem. 2023 Sep;124(9):1404-1422. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Leuk Res. 2022 Sep:120:106920. [Abstract]
- Biochem Biophys Res Commun. 2022 Jan 15:588:147-153. [Abstract]
- Biochem Biophys Rep. 2021 Aug 13:27:101099. [Abstract]
- Biochem Biophys Res Commun. 2018 Sep 26;504(1):231-237. [Abstract]
- Anticancer Res. 2025 Jun;45(6):2285-2295. [Abstract]
- Biomed Chromatogr. 2020 Jun;34(6):e4825. [Abstract]
- STAR Protocols. 2020 Jun 3;1(1):100024. [Abstract]
- Gene Rep. 2026 Jan 3;42:102413.
- University of California, Los Angeles. 2026.
- bioRxiv. 2026 May 25.
- bioRxiv. 2026 Apr 19.
- bioRxiv. 2026 Apr 22:2026.04.19.719504. [Abstract]
- bioRxiv. 2026 Feb 23.
- bioRxiv. 2026 Jan 25.
- bioRxiv. 2025 Nov 3:2025.11.02.685764. [Abstract]
- bioRxiv. 2025 Sep 15.
- Dartmouth College. 2025.
- bioRxiv. 2025 Mar 17:2025.03.14.643359. [Abstract]
- bioRxiv. 2024 Dec 10:2024.12.09.627542. [Abstract]
- Texas Southern University. 2024 July 02.
- bioRxiv. 2024 Nov 15:2024.11.11.623139. [Abstract]
- SSRN. 2023 Sep 29.
- bioRxiv. 2023 Jul 19:2023.07.19.549715. [Abstract]
- bioRxiv. 2023 Jul 17.
- University of Gothenburg. 2023 Jun 27.
- bioRxiv. 2023 Jan 25.
- SSRN. 2022 Nov 21.
- J Oncol. 2022 Jun 23;2022:8724933. [Abstract]
- Department of Biochemistry. 2020 Oct.
- bioRxiv. 2020 Jun.
- Patent. US20200108066A1
- J Oncol. 2019 Jun 2;2019:5952836. [Abstract]
- Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]
- Oncotarget. 2017 Jun 27;8(40):67422-67438. [Abstract]
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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WB
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WB
-
WB
Activité biologique
|
Cdk4/cyclin D1 2 nM (IC50) |
CDK6/cyclinD1 10 nM (IC50) |
CDK9/cyclinT1 57 nM (IC50) |
CDK5/p35 287 nM (IC50) |
Cdk5/p25 355 nM (IC50) |
CDK2/cyclinE 504 nM (IC50) |
CDK1/cyclinB1 1627 nM (IC50) |
CDK7/Mat1/cyclinH1 3910 nM (IC50) |
PIM1 50 nM (IC50) |
PIM2 3400 nM (IC50) |
HIPK2 31 nM (IC50) |
DYRK2 61 nM (IC50) |
CK2 117 nM (IC50) |
GSK3b 192 nM (IC50) |
JNK3 389 nM (IC50) |
FLT3 (D835Y) 403 nM (IC50) |
DRAK1 659 nM (IC50) |
FLT3 3960 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.54 μM
Compound: Ly2835219
|
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 30165341] |
| MCF7 | IC50 |
0.71 μM
Compound: Ly2835219
|
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 30165341] |
| PANC-1 | IC50 |
5.94 μM
Compound: Ly2835219
|
Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay
Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay
|
[PMID: 30165341] |
Abemaciclib (LY2835219) reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1].
Abemaciclib (LY2835219) shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2].
Abemaciclib (LY2835219) inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Abemaciclib (LY2835219) (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1231930-82-7
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Appearance Solid
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Masse moléculaire 602.70
-
Formule C28H36F2N8O3S
-
Color White to yellow
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SMILES
CC(N1C2=CC(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)=CC(F)=C2N=C1C)C.CS(=O)(O)=O
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Synonyms
LY2835219 methanesulfonate
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (125)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Nature
2017 Aug 24;548(7668):471-475. PMID: 28813415
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475. [Abstract]
Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, GW572016, or Abemaciclib for 48 h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500 nM) for 0, 1, or 7 days before exposure to Staurosporine (500 nM) for 4 h.
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Cancer Cell
GABAergic neuronal lineage development determines clinically actionable targets in diffuse hemispheric glioma, H3G34-mutant. [Abstract]2024 Aug 27:S1535-6108(24)00305-2. PMID: 39232581 -
Cell
2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455 -
Cell
2023 Jun 8;186(12):2628-2643.e21. PMID: 37267950 -
Cell
2018 Nov 1;175(4):984-997.e24. PMID: 30388455 -
Cancer Discov
INX-315, a selective CDK2 inhibitor, induces cell cycle arrest and senescence in solid tumors. [Abstract]2024 Mar 1;14(3):446-467. PMID: 38047585 -
Nat Cancer
Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders. [Abstract]2021 Apr;2(4):429-443. PMID: 34568836 -
Nat Metab
2020 Jan;2(1):41-49. PMID: 31993556 -
Bioact Mater
2021 Sep 8:10:247-254. PMID: 34901543 -
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Mol Cell
2025 Sep 4;85(17):3333-3342.e4. PMID: 40858109 -
Cancer Res
Abemaciclib is effective in palbociclib-resistant hormone receptor-positive metastatic breast cancers. [Abstract]2023 Oct 2;83(19):3264-3283. PMID: 37384539 -
Cancer Res
Bcl-xL Enforces a Slow-Cycling State Necessary for Survival in the Nutrient-Deprived Microenvironment of Pancreatic Cancer. [Abstract]2022 May 16;82(10):1890-1908. PMID: 35315913 -
Cancer Res
2019 Oct 15;79(20):5245-5259. PMID: 31395606 -
Mol Cell
2017 Oct 19;68(2):336-349.e6. PMID: 29053957 -
Cancer Res
Kinome-Wide RNA Interference Screen Reveals a Role for PDK1 in Acquired Resistance to CDK4/6 Inhibition in ER-Positive Breast Cancer. [Abstract]2017 May 1;77(9):2488-2499. PMID: 28249908
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2017 May 1;77(9):2488-2499. [Abstract]
Treatment with PD 0332991 and Abemaciclib shows an induction of S241 P-PDK1 as early as 1 h after drug exposure without an increased in total PDK1 protein.
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Cancer Res
2016 Nov 15;76(22):6723-6734. PMID: 27634768
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2016 Nov 15;76(22):6723-6734. [Abstract]
The effects of the CDK inhibitor Abemaciclib, PD 0332991 and Ribocilib on Trop2 ICD cleavage. CDK inhibitors decrease Trop2 ICD abundance after the 2nd day of CDK inhibitor treatment.
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Nat Commun
CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. [Abstract]2026 Jan 22;17(1):619. PMID: 41571637 -
Nat Commun
CDK4 inactivation inhibits apoptosis via mitochondria-ER contact remodeling in triple-negative breast cancer. [Abstract]2025 Jan 9;16(1):541. PMID: 39788939 -
Nat Commun
Targeting the Retinoblastoma/E2F repressive complex by CDK4/6 inhibitors amplifies oncolytic potency of an oncolytic adenovirus. [Abstract]2022 Aug 10;13(1):4689. PMID: 35948546 -
Nat Commun
Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation. [Abstract]2021 Nov 16;12(1):6607. PMID: 34785661 -
Nat Commun
Co-targeting CDK4/6 and AKT with endocrine therapy prevents progression in CDK4/6 inhibitor and endocrine therapy-resistant breast cancer. [Abstract]2021 Aug 25;12(1):5112. PMID: 34433817
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]
MPF-R and TPF-R cells were treated with different concentrations of the CDK4/6 inhibitor (CDK4/6i) Palbociclib (HY-A0065), Ribociclib (HY-15777C) or Abemaciclib (HY-16297A) for 6 days. Cell growth was measured by crystal violet colorimetric assay. Growth relative to vehicle (%) is plotted against log drug concentration.
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Nat Commun
Death effector domain-containing protein induces vulnerability to cell cycle inhibition in triple-negative breast cancer. [Abstract]2019 Jun 28;10(1):2860. PMID: 31253784 -
Nat Commun
CDK4/6 and autophagy inhibitors synergistically induce senescence in Rb positive cytoplasmic cyclin E negative cancers. [Abstract]2017 Jun 27;8:15916. PMID: 28653662 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
Dual Targeting of Tau Kinases and Autophagy by Abemaciclib Independent of CDK4/6 Inhibition. [Abstract]2026 Mar;13(14):e13135. PMID: 41532696 -
Adv Sci (Weinh)
Two-Wave Variable Nanotheranostic Agents for Dual-Mode Imaging-Guided Photo-Induced Triple-Therapy for Cancer. [Abstract]2022 Aug 2;e2201834. PMID: 35918610 -
Adv Sci (Weinh)
Charge and Size Dual Switchable Nanocage for Novel Triple-Interlocked Combination Therapy Pattern. [Abstract]2020 Aug 4;7(18):2000906. PMID: 32999836 -
J Exp Clin Cancer Res
CDK16 promotes the progression and metastasis of triple-negative breast cancer by phosphorylating PRC1. [Abstract]2022 Apr 21;41(1):149. PMID: 35449080 -
J Nanobiotechnology
Inhibition of METTL14 overcomes CDK4/6 inhibitor resistance driven by METTL14-m6A-E2F1-axis in ERα-positive breast cancer. [Abstract]2025 Jan 3;23(1):3. PMID: 39754249 -
Sci Adv
2026 Jun 12;12(24):eaef1962. PMID: 42284392 -
J Biomed Sci
CDK4/6 inhibitors synergize with radiotherapy to prime the tumor microenvironment and enhance the antitumor effect of anti-PD-L1 immunotherapy in triple-negative breast cancer. [Abstract]2025 Aug 20;32(1):79. PMID: 40836337 -
Blood Cancer J
Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c). [Abstract]2022 Jan 11;12(1):5. PMID: 35017466 -
Cell Rep Med
CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. [Abstract]2025 Dec 29:102526. PMID: 41468895 -
Clin Cancer Res
2024 May 8. PMID: 38718141 -
Int J Biol Sci
Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib. [Abstract]2019 Jan 1;15(3):522-532. PMID: 30745839 -
Cell Death Dis
Metformin as a senostatic drug enhances the anticancer efficacy of CDK4/6 inhibitor in head and neck squamous cell carcinoma. [Abstract]2020 Oct 28;11(10):925. PMID: 33116117 -
Cell Death Dis
Absence of cyclin-dependent kinase inhibitor p27 or p18 increases efficiency of iPSC generation without induction of iPSC genomic instability. [Abstract]2019 Mar 20;10(4):271. PMID: 30894510 -
J Pharm Anal
Ursodeoxycholic acid inhibits the uptake of cystine through SLC7A11 and impairs de novo synthesis of glutathione. [Abstract]2025 Jan;15(1):101068. PMID: 39902457 -
Int J Biol Macromol
Molecular interaction of abemaciclib with human serum albumin: Insights from spectroscopy, microscopy, and computational approaches. [Abstract]2025 Dec 9;337(Pt 2):149613. PMID: 41380878 -
Phytomedicine
Resveratrol combats Salmonella infection via liberating vacuole-enclosed bacteria for enhanced autophagic clearance and blocking HMGA2-mediated G2/M arrest. [Abstract]2026 May:154:158042. PMID: 41812383 -
EMBO Mol Med
Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML. [Abstract]2025 Aug 29. PMID: 40883610 -
EMBO J
2024 Dec;43(23):5972-6000. PMID: 39448884 -
EMBO J
2024 Oct;43(19):4406-4436. PMID: 39160273 -
EMBO J
Pharmacological CDK4/6 inhibition reveals a p53-dependent senescent state with restricted toxicity. [Abstract]2022 Mar 15;41(6):e108946. PMID: 34985783 -
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ACS Appl Mater Interfaces
Artificial Assembled Macrophage Co-Deliver Black Phosphorus Quantum Dot and CDK4/6 Inhibitor for Colorectal Cancer Triple-Therapy. [Abstract]2022 May 11;14(18):20628-20640. PMID: 35477252 -
NPJ Precis Oncol
Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]2025 Nov 21;9(1):373. PMID: 41272086
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]
MCL17-PDX mice were treated as indicated: vehicle (n = 5), abemaciclib (50 mg/kg, oral, daily; n = 5), and volasertib (5 mg/kg, intraperitoneal, weekly; n = 5). Tumor size was measured every 7 days during the treatment. Tumor volume = length x width2/2. Mice were euthanized after 21 days of treatment. Tumors were excised and weighed in comparison between each group.
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NPJ Precis Oncol
Acetylation of ELF5 suppresses breast cancer progression by promoting its degradation and targeting CCND1. [Abstract]2021 Mar 19;5(1):20. PMID: 33742100 -
NPJ Breast Cancer
JAK/STAT1-interferon-ISGylation networks in breast cancer resistance to inhibitors of FOXM1 and CDK4/6. [Abstract]2026 Feb 12. PMID: 41680190 -
NPJ Breast Cancer
CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. [Abstract]2025 Dec 3;11(1):135. PMID: 41339342 -
Biomed Pharmacother
A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma. [Abstract]2025 Aug:189:118340. PMID: 40651458 -
Cell Chem Biol
Multiomics Profiling Establishes the Polypharmacology of FDA-Approved CDK4/6 Inhibitors and the Potential for Differential Clinical Activity. [Abstract]2019 Aug 15;26(8):1067-1080.e8. PMID: 31178407 -
Cell Rep
IMPDH2 dephosphorylation under FGFR signaling promotes S-phase progression and tumor growth. [Abstract]2024 Dec 30;44(1):115116. PMID: 39739531 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Cell Rep
BCL-xL inhibition potentiates cancer therapies by redirecting the outcome of p53 activation from senescence to apoptosis. [Abstract]2022 Dec 20;41(12):111826. PMID: 36543138 -
Cell Rep
CDK14 inhibition reduces mammary stem cell activity and suppresses triple negative breast cancer progression. [Abstract]2022 Sep 13;40(11):111331. PMID: 36103813 -
Cell Rep
2017 Oct 31;21(5):1386-1398. PMID: 29091774 -
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J Med Chem
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases. [Abstract]2023 Mar 23;66(6):4106-4130. PMID: 36876904 -
Br J Cancer
Transiently hypoxic tumour cell turnover and radiation sensitivity in human tumour xenografts. [Abstract]2022 Jun;126(11):1616-1626. PMID: 35031765 -
JCI Insight
RB expression confers sensitivity to CDK4/6 inhibitor-mediated radiosensitization across breast cancer subtypes. [Abstract]2022 Feb 8;7(3):e154402. PMID: 34932500 -
Int J Mol Med
2025 Nov;56(5):167. PMID: 40808344 -
Acta Neuropathol Commun
Identifying and exploiting combinatorial synthetic lethality by characterizing adaptive kinome rewiring of EGFRvIII-driven glioblastoma. [Abstract]2025 Jun 28;13(1):143. PMID: 40581663 -
Breast Cancer Res
Estrogen receptor coregulator binding modulator (ERX-11) enhances the activity of CDK4/6 inhibitors against estrogen receptor-positive breast cancers. [Abstract]2019 Dec 26;21(1):150. PMID: 31878959 -
Biochem Pharmacol
Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. [Abstract]2017 Jan 15:124:29-42. PMID: 27816545
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2017 Jan 15:124:29-42. [Abstract]
Effect of LY2835219 on the expression of ABCB1 or ABCG2 in MDR cells. The protein level of ABCB1 and ABCG2 on MDR cells after 0, 0.1, 0.2 and 0.4 μM LY2835219 stimulation for 48h are measured by Western blot analysis, and mRNA level are measured by PCR (GAPDH as loading control).
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Mol Cancer Ther
Harnessing senolytics and PARP inhibition to expand the antitumor activity of CDK4/6 inhibitors in prostate cancer. [Abstract]2025 Jul 2. PMID: 40601842 -
Mol Cancer Ther
AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]2024 Oct 1;23(10):1404-1417. PMID: 38894678 -
Commun Biol
A genome-scale CRISPR Cas9 dropout screen identifies synthetically lethal targets in SRC-3 inhibited cancer cells. [Abstract]2021 Mar 25;4(1):399. PMID: 33767353 -
Cancer Gene Ther
Abemaciclib impairs glioblastoma sphere formation by targeting the GSK3β-mediated transcriptional regulation of CD44 and TCF7L2. [Abstract]2025 Aug 14. PMID: 40813896 -
Int J Mol Sci
Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]2022 Feb 24;23(5):2493. PMID: 35269635 -
Int J Mol Sci
Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs). [Abstract]2021 Jan 8;22(2):575. PMID: 33430060 -
Pharmaceuticals (Basel)
Development and Application of an UPLC-MS/MS Method for Simultaneous Quantification of Abemaciclib and Tamoxifen with Their Active Metabolites in Rat Plasma: Application to a Pharmacokinetic Study. [Abstract]2026 May 19;19(5):795. PMID: 42198468 -
Mol Oncol
Palbociclib induces activation of AMPK and inhibits hepatocellular carcinoma in a CDK4/6-independent manner. [Abstract]2017 Aug;11(8):1035-1049. PMID: 28453226
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]
Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.
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Transl Oncol
TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor developed for the treatment of MTAP-deleted cancers. [Abstract]2025 Jan 3:52:102264. PMID: 39756156 -
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Targeting the mitotic kinase NEK2 enhances CDK4/6 inhibitor efficacy by potentiating genome instability. [Abstract]2025 Jan 16:108196. PMID: 39826695 -
Sci Rep
Selective but not pan-CDK inhibition abrogates 5-FU-driven tissue factor upregulation in colon cancer. [Abstract]2024 May 8;14(1):10582. PMID: 38719932 -
Sci Rep
2022 Jul 20;12(1):12420. PMID: 35859155 -
Sci Rep
Drug-induced PD-L1 expression and cell stress response in breast cancer cells can be balanced by drug combination. [Abstract]2019 Oct 22;9(1):15099. PMID: 31641154 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Biochim Biophys Acta
Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81. [Abstract]2017 Nov 20;1865(2):354-363. PMID: 29157894 -
Heliyon
CDK4/6i enhances the antitumor effect of PD1 antibody by promoting TLS formation in ovarian cancer. [Abstract]2023 Sep 14;9(9):e19760. PMID: 37809574 -
Transl Lung Cancer Res
CDK4/6 inhibitor abemaciclib combined with low-dose radiotherapy enhances the anti-tumor immune response to PD-1 blockade by inflaming the tumor microenvironment in Rb-deficient small cell lung cancer. [Abstract]2024 May 31;13(5):1032-1046. PMID: 38854937 -
Front Oncol
Patient-Derived Xenograft Models for Intrahepatic Cholangiocarcinoma and Their Application in Guiding Personalized Medicine. [Abstract]2021 Jul 13:11:704042. PMID: 34327143 -
Naunyn Schmiedebergs Arch Pharmacol
Piperazine ring toxicity in three novel anti-breast cancer drugs: an in silico and in vitro metabolic bioactivation approach using olaparib as a case study. [Abstract]2023 Jul;396(7):1435-1450. PMID: 36738368 -
Nutrition
β-hydroxy-β-methylbutyrate (HMB) improves mitochondrial function in myocytes through pathways involving PPARβ/δ and CDK4. [Abstract]2019 Apr:60:217-226. PMID: 30677545 -
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Identification of reactive intermediate formation and bioactivation pathways in Abemaciclib metabolism by LC-MS/MS: in vitro metabolic investigation. [Abstract]2019 Jan 23;6(1):181714. PMID: 30800400 -
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Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. [Abstract]2023 Sep;124(9):1404-1422. PMID: 37566640 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
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Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
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Targeting cyclin-dependent kinases 4/6 inhibits survival of megakaryoblasts in acute megakaryoblastic leukaemia. [Abstract]2022 Sep:120:106920. PMID: 35872339 -
Biochem Biophys Res Commun
The CDK4/6-UCHL5-BRD4 axis confers resistance to BET inhibitors in MLL-rearranged leukemia cells by suppressing BRD4 protein degradation. [Abstract]2022 Jan 15:588:147-153. PMID: 34954522 -
Biochem Biophys Rep
Efficacy of a combination therapy targeting CDK4/6 and autophagy in a mouse xenograft model of t(8;21) acute myeloid leukemia. [Abstract]2021 Aug 13:27:101099. PMID: 34430715 -
Biochem Biophys Res Commun
Ploidy-dependent change in cyclin D2 expression and sensitization to cdk4/6 inhibition in human somatic haploid cells. [Abstract]2018 Sep 26;504(1):231-237. PMID: 30193733 -
Anticancer Res
Trametinib Synergized With Abemaciclib to Inhibit Tumor Growth in Human Head and Neck Squamous Cell Carcinoma Cells. [Abstract]2025 Jun;45(6):2285-2295. PMID: 40425343 -
Biomed Chromatogr
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STAR Protocols
Establishment and Use of Patient-Derived Xenograft Models for Drug Testing in Head and Neck Squamous Cell Carcinoma. [Abstract]2020 Jun 3;1(1):100024. PMID: 33111077 -
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bioRxiv
CDK4/6 inhibition sensitizes breast cancer to NK cell therapy by inducing immune-interactive surface proteins. [Abstract]2026 Apr 22:2026.04.19.719504. PMID: 42079201 -
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bioRxiv
2025 Nov 3:2025.11.02.685764. PMID: 41279360 -
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bioRxiv
2025 Mar 17:2025.03.14.643359. PMID: 40166148 -
bioRxiv
2024 Dec 10:2024.12.09.627542. PMID: 39713309 -
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bioRxiv
Therapeutic benefits of maintaining CDK4/6 inhibitors and incorporating CDK2 inhibitors beyond progression in breast cancer. [Abstract]2024 Nov 15:2024.11.11.623139. PMID: 39605351 -
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bioRxiv
2023 Jul 19:2023.07.19.549715. PMID: 37502927 -
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J Oncol
2022 Jun 23;2022:8724933. PMID: 35783158 -
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J Oncol
2019 Jun 2;2019:5952836. PMID: 31275382 -
Oncotarget
The addition of abemaciclib to sunitinib induces regression of renal cell carcinoma xenograft tumors. [Abstract]2017 Jul 27;8(56):95116-95134. PMID: 29221116
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]
Abemaciclib causes increased PARP cleavage in RCC. In 786-O cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134. [Abstract]
Abemaciclib causes increased PARP cleavage in RCC. In Caki-1 cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.
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Oncotarget
GTSE1: a novel TEAD4-E2F1 target gene involved in cell protrusions formation in triple-negative breast cancer cell models. [Abstract]2017 Jun 27;8(40):67422-67438. PMID: 28978043
Abemaciclib methanesulfonate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 27;8(40):67422-67438. [Abstract]
GTSE1 protein and mRNA levels in MDA-MB-157 and MDA-MB-231 cell lines treated respectively with Abemaciclib 0.5 μM for 24h. Data are presented as mean±SEM of three independent experiments.
Solvant et solubilité
H2O : 125 mg/mL (207.40 mM; Need ultrasonic)
DMSO : 10 mg/mL (16.59 mM; ultrasonic and warming and heat to 80°C; 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (4.15 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.15 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: PBS
Solubility: 25 mg/mL (41.48 mM); Clear 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocole
Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between Abemaciclib (LY2835219) and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of < 1 is synergistic and a CI of > 1 is antagonistic.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Six-week-old BALB/c female nude mice are injected subcutaneously with OSC-19 (1×106) cells. When tumor sizes reach approximately 100 mm3, mice are randomized by tumor size and subjected to each treatment. At least 5 mice per treatment group are included. Each group of mice is dosed via daily oral gavage with vehicle, Abemaciclib (LY2835219) (45 mg/kg/d or 90 mg/kg/d), RAD001 (5 mg/kg/d), or a combination of both. The Abemaciclib (LY2835219) is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0). Tumor size and body weight are measured twice weekly. Tumor volumes are calculated using the following formula: V=(L × W2)/2 (L, Length; W, width). Mice are gavaged a final time on day 14 and sacrificed the following day. The tumors are removed for Western blot and immunohistochemistry.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22;7(12):14803-13. [Content Brief]
[2]. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63. [Content Brief]
[3]. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37. [Content Brief]
[4]. Wu T, et al. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15;124:29-42. [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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.6592 mL | 8.2960 mL | 16.5920 mL | 41.4800 mL |
| 5 mM | 0.3318 mL | 1.6592 mL | 3.3184 mL | 8.2960 mL | |
| 10 mM | 0.1659 mL | 0.8296 mL | 1.6592 mL | 4.1480 mL | |
| 15 mM | 0.1106 mL | 0.5531 mL | 1.1061 mL | 2.7653 mL | |
| H2O | 20 mM | 0.0830 mL | 0.4148 mL | 0.8296 mL | 2.0740 mL |
| 25 mM | 0.0664 mL | 0.3318 mL | 0.6637 mL | 1.6592 mL | |
| 30 mM | 0.0553 mL | 0.2765 mL | 0.5531 mL | 1.3827 mL | |
| 40 mM | 0.0415 mL | 0.2074 mL | 0.4148 mL | 1.0370 mL | |
| 50 mM | 0.0332 mL | 0.1659 mL | 0.3318 mL | 0.8296 mL | |
| 60 mM | 0.0277 mL | 0.1383 mL | 0.2765 mL | 0.6913 mL | |
| 80 mM | 0.0207 mL | 0.1037 mL | 0.2074 mL | 0.5185 mL | |
| 100 mM | 0.0166 mL | 0.0830 mL | 0.1659 mL | 0.4148 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.