ChemicalBook CAS DataBase List 2173556-69-7

2173556-69-7

Name	Carbamic acid, N-[5-[2-(acetylamino)-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, cyclohexyl ester
CAS	2173556-69-7
Molecular Formula	C22H24N4O3S
Molecular Weight	424.52
MOL File	2173556-69-7.mol

Chemical Properties

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

Hazard Information

Uses

PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, 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)
T_max (hr)	0.5
C_max (ng/mL)	2423
AUC_0-24 (ng/mL?hr)	4821	1588
AUCINF (ng/mL?hr)	4897	1590
t_1/2 (hr)	1.3	1.0
MRT (hr)	1.8	0.8
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)

storage

Store at -20°C

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

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