SKLB610
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MedKoo CAT#: 401970

CAS#: 1125780-41-7

Description: SKLB610 is a VEGFR inhibitor that potently suppresses human tumor angiogenesis. SKLB610 inhibited angiogenesis-related tyrosine kinase VEGFR2, fibroblast growth factor receptor 2 (FGFR2) and platelet-derived growth factor receptor (PDGFR) at rate of 97%, 65% and 55%, respectively, at concentration of 10μM in biochemical kinase assays. SKLB610 exhibited its antitumor activity as a multi-targeted inhibitor with more potent inhibition of VEGFR2 activity. Its potential to be a candidate of anticancer agent is worth being further investigated.

Chemical Structure

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SKLB610
CAS# 1125780-41-7
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 401970
Name: SKLB610
CAS#: 1125780-41-7
Chemical Formula: C21H16F3N3O3
Exact Mass: 415.11
Molecular Weight: 415.370
Elemental Analysis: C, 60.72; H, 3.88; F, 13.72; N, 10.12; O, 11.56

Price and Availability

Size Price Availability Quantity
100mg USD 650
200mg USD 850
500mg USD 1550
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Synonym: SKLB610; SKLB 610; SKLB-610.

IUPAC/Chemical Name: N-methyl-4-(4-(3-(trifluoromethyl)benzamido)phenoxy)picolinamide

InChi Key: WACDHHMEVMSODJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H16F3N3O3/c1-25-20(29)18-12-17(9-10-26-18)30-16-7-5-15(6-8-16)27-19(28)13-3-2-4-14(11-13)21(22,23)24/h2-12H,1H3,(H,25,29)(H,27,28)

SMILES Code: O=C(NC)C1=NC=CC(OC2=CC=C(NC(C3=CC=CC(C(F)(F)F)=C3)=O)C=C2)=C1

Appearance: white 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, DMF, and ethanol

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

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Product Data:
Product Data
Instruction:
View handling instruction
Biological target: SKLB610 demonstrates potent inhibition of VEGFR2, FGFR2, and PDGFRβ activity at 10 µM, with inhibitions of 97%, 65%, and 55%, respectively. It exhibits selectivity for these targets over PI3K, EGFR, Aurora A, Cdk2/cyclin E, and Cdk6/cyclin D3 at the same concentration. In HUVECs, SKLB610 inhibits VEGFR2 phosphorylation induced by VEGF, hinders HUVEC proliferation induced by VEGF and bFGF (IC50s = 2.2 and 4.7 µM, respectively), and impedes capillary tube formation and migration at concentrations of 2.5 and 10 µM, respectively. Additionally, SKLB610 shows anti-proliferative effects on various cancer cells (IC50s = 5.7, 5.3, 25.6, 6.4, and 6.3 µM for A549, HCT116, MDA-MB-231, Raji, and DU145 cells, respectively).
In vitro activity: SKLB610 has potential to overcome resistance to cytotoxic anticancer drugs, which could benefit patients with multidrug-resistant cancers. Neither ABCB1 nor ABCG2 confered resistance to SKLB610, but SKLB610 selectively sensitized ABCG2-overexpressing multidrug-resistant cancer cells to cytotoxic anticancer agents. SKLB610 reversed ABCG2-mediated MDR by attenuating the drug-efflux function of ABCG2 without affecting its total cell expression. Reference: Biomed Pharmacother. 2022 May;149:112922. https://pubmed.ncbi.nlm.nih.gov/36068781/
In vivo activity: SKLB610 exhibited antitumor activity and has potential to be a candidate of anticancer agent. Chronic intraperitoneally administration of SKLB610 resulted in significant inhibition in the growth of established human A549 and HCT116 tumor xenografts in nude mice without exhibiting toxicity. Histological analysis showed significant reductions in intratumoral microvessel density of 43-55% relative to controls depending on the specific tumor xenografts. Reference: Cell Physiol Biochem. 2011;27(5):565-74. https://pubmed.ncbi.nlm.nih.gov/21691074/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 20.0 48.15
DMSO 16.0 38.52
Ethanol 5.0 12.04

Preparing Stock Solutions

The following data is based on the product molecular weight 415.37 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. Wu CP, Murakami M, Wu YS, Lin CL, Li YQ, Huang YH, Hung TH, Ambudkar SV. The multi-targeted tyrosine kinase inhibitor SKLB610 resensitizes ABCG2-overexpressing multidrug-resistant cancer cells to chemotherapeutic drugs. Biomed Pharmacother. 2022 May;149:112922. doi: 10.1016/j.biopha.2022.112922. Epub 2022 Apr 5. PMID: 36068781; PMCID: PMC10506422. 2. Cao ZX, Zheng RL, Lin HJ, Luo SD, Zhou Y, Xu YZ, Zeng XX, Wang Z, Zhou LN, Mao YQ, Yang L, Wei YQ, Yu LT, Yang SY, Zhao YL. SKLB610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. Cell Physiol Biochem. 2011;27(5):565-74. doi: 10.1159/000329978. Epub 2011 Jun 15. PMID: 21691074.
In vitro protocol: 1. Wu CP, Murakami M, Wu YS, Lin CL, Li YQ, Huang YH, Hung TH, Ambudkar SV. The multi-targeted tyrosine kinase inhibitor SKLB610 resensitizes ABCG2-overexpressing multidrug-resistant cancer cells to chemotherapeutic drugs. Biomed Pharmacother. 2022 May;149:112922. doi: 10.1016/j.biopha.2022.112922. Epub 2022 Apr 5. PMID: 36068781; PMCID: PMC10506422.
In vivo protocol: 1. Cao ZX, Zheng RL, Lin HJ, Luo SD, Zhou Y, Xu YZ, Zeng XX, Wang Z, Zhou LN, Mao YQ, Yang L, Wei YQ, Yu LT, Yang SY, Zhao YL. SKLB610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. Cell Physiol Biochem. 2011;27(5):565-74. doi: 10.1159/000329978. Epub 2011 Jun 15. PMID: 21691074.

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1: Huang Y, Luo X, You X, Xia Y, Song X, Yu L. The preparation and evaluation of water-soluble SKLB610 nanosuspensions with improved bioavailability. AAPS PharmSciTech. 2013 Sep;14(3):1236-43. doi: 10.1208/s12249-013-0005-7. Epub 2013 Aug 10. PubMed PMID: 23934433; PubMed Central PMCID: PMC3755164.

2: Luo X, Li S, Xie Y, He J, Li J, Lin H, Wang N, Yang S, Zhao Y, Yu L, Song X. Pharmacokinetic studies of a novel multikinase inhibitor for treating cancer by HPLC-UV. J Chromatogr Sci. 2013 Jan;51(1):17-20. doi: 10.1093/chromsci/bms098. Epub 2012 Jun 17. PubMed PMID: 22710664.

3: Cao ZX, Zheng RL, Lin HJ, Luo SD, Zhou Y, Xu YZ, Zeng XX, Wang Z, Zhou LN, Mao YQ, Yang L, Wei YQ, Yu LT, Yang SY, Zhao YL. SKLB610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. Cell Physiol Biochem. 2011;27(5):565-74. doi: 10.1159/000329978. Epub 2011 Jun 15. PubMed PMID: 21691074.