SKLB477
featured

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

MedKoo CAT#: 406978

CAS#: 1370256-78-2

Description: SKLB4771, also known as FLT3-IN-1, is a potent and selective FLT3 inhibitor potentially for the treatment of cutaneous inflammation and psoriasis-like symptoms of disease. Mechanistic studies indicated that SKLB4771 treatment significantly decreased the number and activation of pDCs and mDCs in vitro and in vivo, and subsequent T-cell cascade reactions mediated by Th1/Th17 pathways.

Chemical Structure

img
SKLB477
CAS# 1370256-78-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406978
Name: SKLB477
CAS#: 1370256-78-2
Chemical Formula: C25H27N7O3S2
Exact Mass: 537.16
Molecular Weight: 537.660
Elemental Analysis: C, 55.85; H, 5.06; N, 18.24; O, 8.93; S, 11.93

Price and Availability

Size Price Availability Quantity
100mg USD 1250
200mg USD 1950
500mg USD 2850
1g USD 3850
2g USD 5250
5g USD 8250
Bulk inquiry

Synonym: SKLB4771; SKLB-4771; SKLB 4771. FLT3-IN-1; FLT3-IN1; FLT3-IN 1.

IUPAC/Chemical Name: 1-{5-[7-(3- Morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea

InChi Key: LKXFSTAQMOENSC-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H27N7O3S2/c1-17-3-5-18(6-4-17)28-23(33)29-24-30-31-25(37-24)36-22-20-8-7-19(15-21(20)26-16-27-22)35-12-2-9-32-10-13-34-14-11-32/h3-8,15-16H,2,9-14H2,1H3,(H2,28,29,30,33)

SMILES Code: O=C(NC1=CC=C(C)C=C1)NC2=NN=C(SC3=C4C=CC(OCCCN5CCOCC5)=CC4=NC=N3)S2

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:
Product Data
Instruction:
View handling instruction
Biological target: SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.
In vitro activity: To be determined
In vivo activity: Of three highly active compounds, SKLB4771 had the highest in vivo activity against antiacute myeloid leukemia (AML). In an AML MV4-11 xenograft mouse model, a once-daily dose of SKLB4771 at 100 mg/kg for 18 days led to complete tumor regression without obvious toxicity. Reference: J Med Chem. 2012 Apr 26;55(8):3852-66. https://pubmed.ncbi.nlm.nih.gov/22452518/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.3 61.99

Preparing Stock Solutions

The following data is based on the product molecular weight 537.66 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. Yan HX, Li WW, Zhang Y, Wei XW, Fu LX, Shen GB, Yin T, Li XY, Shi HS, Wan Y, Zhang QY, Li J, Yang SY, Wei YQ. Accumulation of FLT3(+) CD11c (+) dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunol Res. 2014 Oct;60(1):112-26. doi: 10.1007/s12026-014-8521-4. PMID: 24895100. 2. Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 Apr 26;55(8):3852-66. doi: 10.1021/jm300042x. Epub 2012 Apr 6. PMID: 22452518.
In vitro protocol: To be determined
In vivo protocol: 1. Yan HX, Li WW, Zhang Y, Wei XW, Fu LX, Shen GB, Yin T, Li XY, Shi HS, Wan Y, Zhang QY, Li J, Yang SY, Wei YQ. Accumulation of FLT3(+) CD11c (+) dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunol Res. 2014 Oct;60(1):112-26. doi: 10.1007/s12026-014-8521-4. PMID: 24895100. 2. Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 Apr 26;55(8):3852-66. doi: 10.1021/jm300042x. Epub 2012 Apr 6. PMID: 22452518.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Yan HX, Li WW, Zhang Y, Wei XW, Fu LX, Shen GB, Yin T, Li XY, Shi HS, Wan Y,
Zhang QY, Li J, Yang SY, Wei YQ. Accumulation of FLT3(+) CD11c (+) dendritic
cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3
inhibitor. Immunol Res. 2014 Oct;60(1):112-26. doi: 10.1007/s12026-014-8521-4.
PubMed PMID: 24895100.