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NVP-CLR457

CAS No. : 1453082-52-4

MCE 站：NVP-CLR457

产品活性：NVP-CLR457 (compound 40) 是一种口服有效的和平衡的泛 I 类 PI3K 抑制剂。NVP-CLR457 显示出明显的剂量依赖性 PK / PD / 疗效关系。NVP-CLR457 具有抗肿瘤活性。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: NVP-CLR457 (compound 40) shows the mTOR activity, with an IC₅₀ of 2474 ± 722 nM, ａnd inhibits RPS6 phosphorylation with an IC₅₀ of 1633 ± 54 nM.
NVP-CLR457 has no impact on the DDR response at concentrations of 1 ａnd 5 μM.
NVP-CLR457 has no effect on the rate of microtubule polymerization.

In Vivo: NVP-CLR457 (compound 40) (athymic nude mice bearing xenotransplanted Rat1-myr-p110α tumors, 3-20 mg/kg, PO, daily for 8 days) shows a dose-dependent inhibition of tumor growth.
NVP-CLR457 (Mice bearing xenograft HBRX2524 human primary breast tumor, 40 mg/kg, PO, daily for 15 days) inhibits the tumor growth throughout the study.
NVP-CLR457 (male Sprague-Dawley rats, 1.0 mg/kg, IV; 3.0 mg/kg, PO; once) shows high level of oral exposure ａnd bioavailability.
Pharmacokinetic Parameters of NVP-CLR457 in male Sprague-Dawley rats.

compound	40
CL (mL/min/kg)	22 ± 6
Vss (L/kg)	4.4 ± 0.2
t1/2 (h)	3.3 ± 0.2
AUC iv (nM*h)	1770 ± 443
oral F (%)	97 ± 20
HDM FA (%)	37

NVP-CLR457 (3 mg/kg (IV) ａnd 10 mg/kg (PO) for female OF1 mice, 0.1 mg/kg (IV), 0.3 mg/kg (PO) for male beagle dogs, once) shows low clearance, moderate volume of distribution, ａnd rapid absorption leading to moderate to long half-lives ａnd high oral bioavailability.
Pharmacokinetic Parameters of NVP-CLR457 in female OF1 mice ａnd male beagle dogs.

species	mouse	dog
PPB (%)	76	71
CL (mL/min/kg)	10	3 ± 0
Vss (L/kg)	2	1.5 ± 0.2
t1/2 (h)	2	11 ± 3
AUC iv (nM*h)	3580	11213 ± 1169
AUC po (nM*h)	1738	11034 ± 1531
oral F (%)	49	98 ± 14
Cmax (nM)	422	1121 ± 128
Tmax (h)	0.5	1.3 ± 0.6

NVP-CLR457 (0.3-100 mg/kg, PO, once) leads to under-proportional increases in exposure (both AUC ａnd Cmax) ａnd much longer Tmax values.
Pharmacokinetic Parameters of NVP-CLR457 in male Sprague Dawley rats, male beagle dogs.

species	rat			dog
dose (mg/kg)	3	30	100	0.3	3
AUC (nM*h)	1709 ± 362	913 ± 251	784 ± 342	12,970 ± 1828	11,213 ± 1169
Cmax (nM)	213 ± 61	41 ± 6	22 ± 4	1121 ± 128	309 ± 40
Tmax (h)	0.5-2	424	24	1-2	2-24

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