SKLB1002 | CAS#1225451-84-2 | MedKoo Biosciences

MedKoo Cat#: 401980 | Name: SKLB1002

Description:

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

SKLB1002 is a new potent VEGFR2 inhibitor, which could significantly inhibit HUVEC proliferation, migration, invasion, and tube formation. Western blot analysis was conducted, which indicated that SKLB1002 inhibited VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal-regulated kinase, focal adhesion kinase, and Src. In vivo zebrafish model experiments showed that SKLB1002 remarkably blocked the formation of intersegmental vessels in zebrafish embryos. SKLB1002 inhibits angiogenesis and may be a potential drug candidate in anticancer therapy.

Chemical Structure

SKLB1002

CAS#1225451-84-2

Theoretical Analysis

MedKoo Cat#: 401980

Name: SKLB1002

CAS#: 1225451-84-2

Chemical Formula: C13H12N4O2S2

Exact Mass: 320.0402

Molecular Weight: 320.39

Elemental Analysis: C, 48.73; H, 3.78; N, 17.49; O, 9.99; S, 20.02

Price and Availability

Size	Price	Availability
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Synonym

SKLB1002; SKLB 1002; SKLB1002.

IUPAC/Chemical Name

2-((6,7-dimethoxyquinazolin-4-yl)thio)-5-methyl-1,3,4-thiadiazole

InChi Key

RQVGFDBMONQTBC-UHFFFAOYSA-N

InChi Code

InChI=1S/C13H12N4O2S2/c1-7-16-17-13(20-7)21-12-8-4-10(18-2)11(19-3)5-9(8)14-6-15-12/h4-6H,1-3H3

SMILES Code

CC1=NN=C(SC2=C3C=C(OC)C(OC)=CC3=NC=N2)S1

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 chloroform

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

Product Data

Instruction

View handling instruction

Biological target:

SKLB1002 is a VEGFR2 inhibitor (IC50 = 32 nM). It is selective for VEGFR2 over a panel of 16 additional kinases (IC50s = 619->10,000 nM).

In vitro activity:

Selective inhibition of VEGFR‑2 through SKLB1002 administration is a promising therapy for ocular angiogenesis. SKLB1002 inhibited endothelial angiogenic functions by blocking the phosphorylation of ERK1/2, JNK and p38. SKLB1002 significantly reduced endothelial cell proliferation, migration and tube formation. Reference: Mol Med Rep. 2020 Jun;21(6):2571-2579. https://pubmed.ncbi.nlm.nih.gov/32323773/

In vivo activity:

SKLB1002 may be a potential drug candidate in anticancer therapy. Zebrafish model experiments showed that SKLB1002 blocked the formation of intersegmental vessels in zebrafish embryos. SKLB1002 inhibited a new microvasculature in zebrafish embryos induced by inoculated tumor cells. Finally, compared with the solvent control, administration of SKLB1002 reached more than 60% inhibition against human tumor xenografts in athymic mice. Reference: Clin Cancer Res. 2011 Jul 1;17(13):4439-50. https://pubmed.ncbi.nlm.nih.gov/21622720/

	Solvent	mg/mL	mM	comments
Solubility
	Chloroform	30.0	93.64

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 320.39 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

Formulation protocol:

1. Zhang QY, Tao SY, Lu C, Li JJ, Li XM, Yao J, Jiang Q, Yan B. SKLB1002, a potent inhibitor of VEGF receptor 2 signaling, inhibits endothelial angiogenic function in vitro and ocular angiogenesis in vivo. Mol Med Rep. 2020 Jun;21(6):2571-2579. doi: 10.3892/mmr.2020.11056. Epub 2020 Apr 6. PMID: 32323773; PMCID: PMC7185286. 2. Nie W, Ma XL, Sang YX, Li YL, Gao X, Xu GC, Shen GB, Shi HS, Liu XX, Wang FT, Wei YQ. Synergic antitumor effect of SKLB1002 and local hyperthermia in 4T1 and CT26. Clin Exp Med. 2014 May;14(2):203-13. doi: 10.1007/s10238-012-0225-2. Epub 2012 Dec 21. PMID: 23263406. 3. Abdelsaid M, Coucha M, Hafez S, Yasir A, Johnson MH, Ergul A. Enhanced VEGF signalling mediates cerebral neovascularisation via downregulation of guidance protein ROBO4 in a rat model of diabetes. Diabetologia. 2017 Apr;60(4):740-750. doi: 10.1007/s00125-017-4214-6. Epub 2017 Jan 23. PMID: 28116460; PMCID: PMC5342922. 4. Zhang S, Cao Z, Tian H, Shen G, Ma Y, Xie H, Liu Y, Zhao C, Deng S, Yang Y, Zheng R, Li W, Zhang N, Liu S, Wang W, Dai L, Shi S, Cheng L, Pan Y, Feng S, Zhao X, Deng H, Yang S, Wei Y. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res. 2011 Jul 1;17(13):4439-50. doi: 10.1158/1078-0432.CCR-10-3109. Epub 2011 May 27. PMID: 21622720.

In vitro protocol:

In vivo protocol:

1. Abdelsaid M, Coucha M, Hafez S, Yasir A, Johnson MH, Ergul A. Enhanced VEGF signalling mediates cerebral neovascularisation via downregulation of guidance protein ROBO4 in a rat model of diabetes. Diabetologia. 2017 Apr;60(4):740-750. doi: 10.1007/s00125-017-4214-6. Epub 2017 Jan 23. PMID: 28116460; PMCID: PMC5342922. 2. Zhang S, Cao Z, Tian H, Shen G, Ma Y, Xie H, Liu Y, Zhao C, Deng S, Yang Y, Zheng R, Li W, Zhang N, Liu S, Wang W, Dai L, Shi S, Cheng L, Pan Y, Feng S, Zhao X, Deng H, Yang S, Wei Y. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res. 2011 Jul 1;17(13):4439-50. doi: 10.1158/1078-0432.CCR-10-3109. Epub 2011 May 27. PMID: 21622720.

1: Nie W, Ma XL, Sang YX, Li YL, Gao X, Xu GC, Shen GB, Shi HS, Liu XX, Wang FT, Wei YQ. Synergic antitumor effect of SKLB1002 and local hyperthermia in 4T1 and CT26. Clin Exp Med. 2012 Dec 21. [Epub ahead of print] PubMed PMID: 23263406. 2: Shen G, Li Y, Du T, Shi G, Dai L, Chen X, Zheng R, Li W, Su X, Zhang S, Wei Y, Yang S, Deng H. SKLB1002, a novel inhibitor of VEGF receptor 2 signaling, induces vascular normalization to improve systemically administered chemotherapy efficacy. Neoplasma. 2012;59(5):486-93. doi: 10.4149/neo_2012_062. PubMed PMID: 22668017. 3: Zhang S, Cao Z, Tian H, Shen G, Ma Y, Xie H, Liu Y, Zhao C, Deng S, Yang Y, Zheng R, Li W, Zhang N, Liu S, Wang W, Dai L, Shi S, Cheng L, Pan Y, Feng S, Zhao X, Deng H, Yang S, Wei Y. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res. 2011 Jul 1;17(13):4439-50. doi: 10.1158/1078-0432.CCR-10-3109. Epub 2011 May 27. PubMed PMID: 21622720.