MedKoo Cat#: 530926 | Name: Lin281632
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lin28 1632, is a RNA binding protein Lin28 inhibitor. Lin281632 promotes mESC differentiation. Lin281632 is also bromodomain inhibitor.

Chemical Structure

Lin281632
Lin281632
CAS#108825-65-6

Theoretical Analysis

MedKoo Cat#: 530926

Name: Lin281632

CAS#: 108825-65-6

Chemical Formula: C15H15N5O

Exact Mass: 281.1277

Molecular Weight: 281.32

Elemental Analysis: C, 64.04; H, 5.37; N, 24.90; O, 5.69

Price and Availability

Size Price Availability Quantity
10mg USD 295.00 2 Weeks
50mg USD 850.00 2 Weeks
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Synonym
Lin28 1632; Lin-28 1632; Lin 28 163; Lin281632; Lin-281632; Lin 281632.
IUPAC/Chemical Name
N-Methyl-N-[3-(3-methyl-1,2,4-triazolo[4,3-b]pyridazin-6-yl)phenyl]acetamide
InChi Key
WPAQLESUVYGUJZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H15N5O/c1-10-16-17-15-8-7-14(18-20(10)15)12-5-4-6-13(9-12)19(3)11(2)21/h4-9H,1-3H3
SMILES Code
CC(N(C)C1=CC=CC(C2=NN3C(C=C2)=NN=C3C)=C1)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
Lin28-let-7 antagonist 1 (compound 1632) is a potent antagonist of Lin28/pre-let-7 interaction.
In vitro activity:
This study tested 16,000 molecules and identified N-methyl-N-[3-(3-methyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)phenyl]acetamide (Lin28-let-7 antagonist 1), which blocked the Lin28/let-7 interaction, rescued let-7 processing and function in Lin28-expressing cancer cells, induced differentiation of mouse embryonic stem cells, and reduced tumor-sphere formation by 22Rv1 and Huh7 cells. Reference: ACS Chem Biol. 2016 Oct 21;11(10):2773-2781. https://pubmed.ncbi.nlm.nih.gov/27548809/
In vivo activity:
This study found that treatment with a LIN28 inhibitor, the small compound C1632, increases let-7 and suppresses PD-L1 expression, leading to reactivation of antitumor immunity in vitro and in vivo. In addition, C1632 also displayed the capacity to inhibit cancer cell proliferation and tumor growth in mice. Reference: Cancer Immunol Res. 2019 Mar;7(3):487-497. https://pubmed.ncbi.nlm.nih.gov/30651289/
Solvent mg/mL mM comments
Solubility
DMSO 28.1 100.00
Ethanol 28.1 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 281.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Patra T, Cunningham DM, Meyer K, Toth K, Ray RB, Heczey A, Ray R. Targeting Lin28 axis enhances glypican-3-CAR T cell efficacy against hepatic tumor initiating cell population. Mol Ther. 2023 Jan 6:S1525-0016(23)00002-3. doi: 10.1016/j.ymthe.2023.01.002. Epub ahead of print. PMID: 36609146. 2. Roos M, Pradère U, Ngondo RP, Behera A, Allegrini S, Civenni G, Zagalak JA, Marchand JR, Menzi M, Towbin H, Scheuermann J, Neri D, Caflisch A, Catapano CV, Ciaudo C, Hall J. A Small-Molecule Inhibitor of Lin28. ACS Chem Biol. 2016 Oct 21;11(10):2773-2781. doi: 10.1021/acschembio.6b00232. Epub 2016 Aug 22. PMID: 27548809. 3. Chen JY, Chen YJ, Liu L, Jin XX, Shen Z, Chen WB, Yang T, Xu SB, Wang GB, Cheng YN, Cheng DZ, Liu ZG, Zheng XH. C1632 suppresses the migration and proliferation of non-small-cell lung cancer cells involving LIN28 and FGFR1 pathway. J Cell Mol Med. 2022 Jan;26(2):422-435. doi: 10.1111/jcmm.17094. Epub 2021 Dec 16. PMID: 34913237; PMCID: PMC8743659. 4. Chen Y, Xie C, Zheng X, Nie X, Wang Z, Liu H, Zhao Y. LIN28/let-7/PD-L1 Pathway as a Target for Cancer Immunotherapy. Cancer Immunol Res. 2019 Mar;7(3):487-497. doi: 10.1158/2326-6066.CIR-18-0331. Epub 2019 Jan 16. PMID: 30651289.
In vitro protocol:
1. Patra T, Cunningham DM, Meyer K, Toth K, Ray RB, Heczey A, Ray R. Targeting Lin28 axis enhances glypican-3-CAR T cell efficacy against hepatic tumor initiating cell population. Mol Ther. 2023 Jan 6:S1525-0016(23)00002-3. doi: 10.1016/j.ymthe.2023.01.002. Epub ahead of print. PMID: 36609146. 2. Roos M, Pradère U, Ngondo RP, Behera A, Allegrini S, Civenni G, Zagalak JA, Marchand JR, Menzi M, Towbin H, Scheuermann J, Neri D, Caflisch A, Catapano CV, Ciaudo C, Hall J. A Small-Molecule Inhibitor of Lin28. ACS Chem Biol. 2016 Oct 21;11(10):2773-2781. doi: 10.1021/acschembio.6b00232. Epub 2016 Aug 22. PMID: 27548809.
In vivo protocol:
1. Chen JY, Chen YJ, Liu L, Jin XX, Shen Z, Chen WB, Yang T, Xu SB, Wang GB, Cheng YN, Cheng DZ, Liu ZG, Zheng XH. C1632 suppresses the migration and proliferation of non-small-cell lung cancer cells involving LIN28 and FGFR1 pathway. J Cell Mol Med. 2022 Jan;26(2):422-435. doi: 10.1111/jcmm.17094. Epub 2021 Dec 16. PMID: 34913237; PMCID: PMC8743659. 2. Chen Y, Xie C, Zheng X, Nie X, Wang Z, Liu H, Zhao Y. LIN28/let-7/PD-L1 Pathway as a Target for Cancer Immunotherapy. Cancer Immunol Res. 2019 Mar;7(3):487-497. doi: 10.1158/2326-6066.CIR-18-0331. Epub 2019 Jan 16. PMID: 30651289.