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Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester

Product Name
Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester
CAS No.
2173556-69-7
Chemical Name
Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester
Synonyms
PK68;PK68, 10 mM in DMSO;Cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate;Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester;Inhibitor,inflammatory,RIPK,oral,Receptor-interacting protein kinases,RIP kinase,cancer,type II inhibitor,PK68,PK-68,inhibit,receptor-interacting kinase 1 (RIPK1),PK 68,TNF
CBNumber
CB35516718
Molecular Formula
C22H24N4O3S
Formula Weight
424.52
MOL File
2173556-69-7.mol
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Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester Property

Density 
1.33±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: 30 mg/mL (70.67 mM)
form 
Solid
pka
10.27±0.70(Predicted)
color 
Off-white to light yellow
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Hazard and Precautionary Statements (GHS)

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Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester Chemical Properties,Usage,Production

Uses

PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis[1].

in vivo

PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice[1].
PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome[1].
PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis[1].

Animal Model:C57BL/6 mice[1]
Dosage:5 mg/kg, 25 mg/kg
Administration:5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days
Result:Exhibited favorable pharmacokinetic profiles and no obvious toxicity in mice treated with a 14-day course at a dose of 25 mg/kg.
Animal Model:C57BL/6 mice[1]
Dosage:2 mg/kg, 10 mg/kg
Administration:2 mg/kg, i.v.; 10 mg/kg, p.o; for 14 days
Result:
PO (Gavage)IV (Bolus)
Tmax (hr)0.5
Cmax (ng/mL)2423
AUC0-24 (ng/mLhr)48211588
AUCINF (ng/mLhr)48971590
t1/2 (hr)1.31.0
MRT (hr)1.80.8
CL (mL/hr/kg)1258
CL (mL/min/kg)21
Vss (mL/kg)1009
Vss (L/kg)1.0
F(%)61
Animal Model:C57BL/6 mice[1]
Dosage:1 mg/kg
Administration:1 mg/kg, i.p.
Result:Provided effective protection against TNFα-induced lethal shock.
Animal Model:C57BL/6 mice[1]
Dosage:5 mg/kg
Administration:5 mg/kg, i.v.
Result:Significantly reduced the number of pulmonary metastasis nodules, decreased lung metastasis, decreased number of RFP-LL/2 cells, attenuated transmigration of RFP-LL/2 cells through the endothelial cell monolayer and had no obvious influence on the proliferation rate and invasion ability of B16-F10 or RFP-LL/2 cells without the endothelial cell monolayer in vitro.

IC 50

RIPK1: 90 nM (IC50); RIPK1: 23 nM (EC50)

References

[1] Jue Hou, et al. Discovery of potent necroptosis inhibitors targeting RIPK1 kinase activity for the treatment of inflammatory disorder and cancer metastasis. Cell Death Dis. 2019 Jun 24;10(7):493. DOI:10.1038/s41419-019-1735-6

Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester Preparation Products And Raw materials

Raw materials

Preparation Products

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Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester Suppliers

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2173556-69-7, Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl esterRelated Search:


  • Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester
  • PK68
  • Inhibitor,inflammatory,RIPK,oral,Receptor-interacting protein kinases,RIP kinase,cancer,type II inhibitor,PK68,PK-68,inhibit,receptor-interacting kinase 1 (RIPK1),PK 68,TNF
  • Cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate
  • PK68, 10 mM in DMSO
  • 2173556-69-7