SML1832
DDR1 Inhibitor 7rh
≥98% (HPLC), discoidin domain receptor-1 inhibitor, powder
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Synonym(s):
4-Ethyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)-phenyl)-3-(pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide, 7rh
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| Size/SKU | Availability | Price |
|---|---|---|
5 mg | Please contact Customer Service for Availability | 3 340,00 CZK |
25 mg | Please contact Customer Service for Availability | 13 600,00 CZK |
About This Item
Product Name
DDR1 Inhibitor 7rh, ≥98% (HPLC)
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C(NC1=CC(C(F)(F)F)=CC(CN2CCN(C)CC2)=C1)C3=CC=C(CC)C(C#CC4=CN5C(N=C4)=CC=N5)=C3
InChI
1S/C30H29F3N6O/c1-3-23-6-7-25(16-24(23)5-4-21-18-34-28-8-9-35-39(28)20-21)29(40)36-27-15-22(14-26(17-27)30(31,32)33)19-38-12-10-37(2)11-13-38/h6-9,14-18,20H,3,10-13,19H2,1-2H3,(H,36,40)
InChI key
DDLPXZXBWGJRGK-UHFFFAOYSA-N
General description
Biochem/physiol Actions
Compound 7rh is a potent, high affinity (Kd =0.6 nM), ATP-competitive inhibitor against discoidin domain-containing receptor 1 (DDR1; IC50 = 6.8 nM, [ATP] = 100 nM) with significantly reduced potency toward 455 other kinases, including DDR2, Bcr-abl, and c-Kit (IC50 = 101.4 nM, 355 nM and >10 μM, respectively). Inhibitor 7rh reduces DDR1 expression/phosphorylation and downstream signaling in a dose-dependent manner (0.1-2 μM; NCI-H23 NSCLCs), effectively suppressing human cancer cells proliferation (IC50 from 38 nM/K562 to 2.98 μM/NCI-H460) and colony formation (IC50 = 0.56 μM/NCI-H23). Inhibitor 7rh is orally availabe in rats and mice (T1/2 = 15.53 h; Tmax = 4.25 h; Cmax = 1867.5 μg/L, F = 67.4%; 25 mg/kg; rats) and displays in vivo efficacy against Kras (LSLG12Vgeo) tumor growth in mice (50 mg/kg/day p.o.).
1 of 1
This Item | |||
|---|---|---|---|
| description ≥98% (HPLC) | description ≥98% (HPLC) | description solid | description The MPS1 Inhibitor, NMS-P715 controls the biological activity of MPS1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) |
| form powder | form powder | form solid | form powder |
| Quality Level 100 | Quality Level - | Quality Level 200 | Quality Level 100 |
| storage temp. 2-8°C | storage temp. 2-8°C | storage temp. −20°C | storage temp. 2-8°C |
| solubility DMSO: 10 mg/mL, clear | solubility DMSO: 2 mg/mL, clear | solubility 0.1 M NaOH: slightly soluble, ethanol: soluble, ethyl acetate: soluble, H2O: insoluble, DMSO: soluble, 0.1 M HCl: slightly soluble | solubility DMSO: 10 mg/mL, clear, colorless |
| color white to beige | color white to beige | color pale yellow | color white |
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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