SIM010603 | CAS#1032265-67-0 | MedKoo Biosciences

MedKoo Cat#: 401915 | Name: SIM010603

Description:

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

SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.

Chemical Structure

SIM010603

CAS#1032265-67-0

Theoretical Analysis

MedKoo Cat#: 401915

Name: SIM010603

CAS#: 1032265-67-0

Chemical Formula: C22H25FN4O2

Exact Mass: 396.1962

Molecular Weight: 396.46

Elemental Analysis: C, 66.65; H, 6.36; F, 4.79; N, 14.13; O, 8.07

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.

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Related CAS #

No Data

Synonym

SIM010603; SIM 010603; SIM-010603

IUPAC/Chemical Name

(Z)-N-(2-(dimethylamino)ethyl)-7-(5-fluoro-2-oxoindolin-3-ylidene)-2-methyl-4,5,6,7-tetrahydro-1H-indole-3-carboxamide

InChi Key

CARLZFLTQJQGIP-CYVLTUHYSA-N

InChi Code

InChI=1S/C22H25FN4O2/c1-12-18(21(28)24-9-10-27(2)3)14-5-4-6-15(20(14)25-12)19-16-11-13(23)7-8-17(16)26-22(19)29/h7-8,11,25H,4-6,9-10H2,1-3H3,(H,24,28)(H,26,29)/b19-15-

SMILES Code

O=C(C1=C(C)NC2=C1CCC/C2=C3C(NC4=C/3C=C(F)C=C4)=O)NCCN(C)C

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

Although SIM010603 exhibited lower activity in regard to proliferation of NCI-H460, MDA-MB-435, and T241-VEGF-A cells (IC(50) > 1 μmol/l), SIM010603 inhibited tumor growth in these xenograft tumor growth models. SIM010603 reduced tumor MVD in T241-VEGF-A tumor xenograft models and decreased positive signals of CD31, NG2 in MDA-MB-435, and LLC-SW-44 xenograft tumor models. (source: Cancer Chemother Pharmacol. 2012 Jan;69(1):173-83) (last updated: 6/23/2015)

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 396.46 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: Wang D, Tang F, Wang S, Jiang Z, Zhang L. Preclinical anti-angiogenesis and anti-tumor activity of SIM010603, an oral, multi-targets receptor tyrosine kinases inhibitor. Cancer Chemother Pharmacol. 2012 Jan;69(1):173-83. doi: 10.1007/s00280-011-1681-1. Epub 2011 Jun 3. PubMed PMID: 21638122.