FN-1501 | CAS#1429515-59-2 | FLT3/CDKs kinase inhibitor

MedKoo Cat#: 206944 | Name: FN-1501

Description:

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

FN-1501 is a potent a FLT3/CDKs kinase inhibitor with potential high efficiency against acute myelocytic leukemia (AML). FN-1501, which possesses potent inhibitory activities against FLT3, CDK2, CDK4, and CDK6 with IC50 values in the nanomolar range, shows antiproliferative activities against MV4-11 cells (IC50: 0.008 μM), which correlates with the suppression of retinoblastoma phosphorylation, FLT3, ERK, AKT, and STAT5 and the onset of apoptosis. Acute-toxicity studies in mice show that FN-1501 (LD50: 186 mg/kg) is safer than AT7519 (32 mg/kg). In MV4-11 xenografts in a nude-mouse model, FN-1501 can induce tumor regression at the dose of 15 mg/kg, which is more efficient than cytarabine (50 mg/kg).

Chemical Structure

FN-1501

CAS#1429515-59-2

Theoretical Analysis

MedKoo Cat#: 206944

Name: FN-1501

CAS#: 1429515-59-2

Chemical Formula: C22H25N9O

Exact Mass: 431.2182

Molecular Weight: 431.50

Elemental Analysis: C, 61.24; H, 5.84; N, 29.21; O, 3.71

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

FN-1501; FN 1501; FN1501

IUPAC/Chemical Name

4‑((7H‑Pyrrolo[2,3‑d]pyrimidin-4-yl)amino)‑N‑(4-((4-methylpiperazin-1-yl)methyl)phenyl)‑1H‑pyrazole-3-carboxamide

InChi Key

VXLAKHWYGRKCGI-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H25N9O/c1-30-8-10-31(11-9-30)13-15-2-4-16(5-3-15)27-22(32)19-18(12-26-29-19)28-21-17-6-7-23-20(17)24-14-25-21/h2-7,12,14H,8-11,13H2,1H3,(H,26,29)(H,27,32)(H2,23,24,25,28)

SMILES Code

O=C(C1=NNC=C1NC2=C3C(NC=C3)=NC=N2)NC4=CC=C(CN5CCN(C)CC5)C=C4

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 431.50 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.

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

1: Zou D, Hu B, Feng S, Si R, Zhong B, Shen B, Du Y, Feng J. FN-1501 Inhibits Diffuse Large B-Cell Lymphoma Tumor Growth by Inducing Cell Cycle Arrest and Apoptosis. Anticancer Agents Med Chem. 2024;24(20):1501-1513. doi: 10.2174/0118715206345788240902062910. PMID: 39229996. 2: Zhang M, Huang MN, Dong XD, Cui QB, Yan Y, She ML, Feng WG, Zhao XS, Wang DT. Overexpression of ABCB1 confers resistance to FLT3 inhibitor FN-1501 in cancer cells: in vitro and in vivo characterization. Am J Cancer Res. 2023 Dec 15;13(12):6026-6037. PMID: 38187048; PMCID: PMC10767331. 3: Richardson GE, Al-Rajabi R, Uprety D, Hamid A, Williamson SK, Baranda J, Mamdani H, Lee YL, Nitika, Li L, Wang X, Dong X. A Multicenter, Open-Label, Phase I/II Study of FN-1501 in Patients with Advanced Solid Tumors. Cancers (Basel). 2023 Apr 29;15(9):2553. doi: 10.3390/cancers15092553. PMID: 37174019; PMCID: PMC10177510. 4: Kumarasamy V, Gao Z, Zhao B, Jiang B, Rubin SM, Burgess K, Witkiewicz AK, Knudsen ES. PROTAC-mediated CDK degradation differentially impacts cancer cell cycles due to heterogeneity in kinase dependencies. Br J Cancer. 2023 Oct;129(8):1238-1250. doi: 10.1038/s41416-023-02399-4. Epub 2023 Aug 25. PMID: 37626264; PMCID: PMC10575895. 5: Wang Y, Zhi Y, Jin Q, Lu S, Lin G, Yuan H, Yang T, Wang Z, Yao C, Ling J, Guo H, Li T, Jin J, Li B, Zhang L, Chen Y, Lu T. Discovery of 4-((7H-Pyrrolo[2,3- d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H- pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518. doi: 10.1021/acs.jmedchem.7b01261. Epub 2018 Feb 12. PMID: 29357250. 6: Zou H, Deirawan H, Uprety D, Daveluy S. Sclerodermatous eruption in a patient with metastatic colon cancer treated with an FLT3/CDK inhibitor. Australas J Dermatol. 2023 Aug;64(3):e272-e274. doi: 10.1111/ajd.14093. Epub 2023 May 31. PMID: 37255338. 7: Zhi Y, Li H, Yang P, Jin Q, Yao C, Li B, Ling J, Guo H, Li T, Jin J, Wang Y, Chen Y, Lu T, Lu S. Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4- (piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor. Eur J Med Chem. 2023 Aug 5;256:115448. doi: 10.1016/j.ejmech.2023.115448. Epub 2023 May 3. PMID: 37163951. 8: Yang J, Friedman R. Synergy and antagonism between azacitidine and FLT3 inhibitors. Comput Biol Med. 2024 Feb;169:107889. doi: 10.1016/j.compbiomed.2023.107889. Epub 2023 Dec 21. PMID: 38199214. 9: Zhi Y, Wang Z, Yao C, Li B, Heng H, Cai J, Xiang L, Wang Y, Lu T, Lu S. Design and Synthesis of 4-(Heterocyclic Substituted Amino)-1H-Pyrazole-3-Carboxamide Derivatives and Their Potent Activity against Acute Myeloid Leukemia (AML). Int J Mol Sci. 2019 Nov 15;20(22):5739. doi: 10.3390/ijms20225739. PMID: 31731727; PMCID: PMC6887723. 10: Lin B, Li Y, Wang T, Qiu Y, Chen Z, Zhao K, Lu N. CRMP2 is a therapeutic target that suppresses the aggressiveness of breast cancer cells by stabilizing RECK. Oncogene. 2020 Sep;39(37):6024-6040. doi: 10.1038/s41388-020-01412-x. Epub 2020 Aug 10. PMID: 32778769.