Ipatasertib (GDC-0068) 1001264-89-6 1001264-89-6

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Molecular Weight: 458 Ipatasertib (GDC-0068) is a highly selective pan-Akt Inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA. Phase 2.

Testing against a broad panel of 230 kinases, GDC-0068 only inhibits 3
kinases by >70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K,
with IC50 of 98 nM, 69 nM, and 860 nM, respectively). GDC-0068 displays
>100-fold selectivity for Akt over PKA with IC50 of 3.1 μM. In LNCaP,
PC3 and BT474M1 cells, GDC-0068 treatment inhibits the phosphorylation
of the Akt substrate, PRAS40 with IC50 of 157 nM, 197 nM, and 208 nM,
respectively. Furthermore, GDC-0068 selectively inhibits Cell Cycle
progression and viability of cancer cell lines driven by Akt signaling,
including those with defects in the tumor suppressor PTEN, oncogenic
mutations in PIK3CA, and amplification of HER2, with strongest effects
in HER2+ and Luminal subtypes.





Oral administration of GDC-0068 in PC3 prostate tumor xenografts model
induces down-regulation of p-PRAS40. In BT474-Tr xenografts, GDC-0068
treatment reduces pS6 and peIF4G levels, re-localizes FOXO3a to nucleus,
and induces feedback upregulation of HER3 and pERK. Administration of
GDC-0068 exhibits potent antitumor efficacy in multiple xenograft tumor
models, including the PTEN-deficient prostate cancer models LNCaP and
PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and
MCF7-neo/HER2 tumor model.

Animal Models	Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
Formulation	Formulated in 0.5% methylcellulose/0.2% Tween-80
Dosages	~100 mg/kg/day
Administration	Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	458
Formula	C24H32ClN5O2
CAS No.	1001264-89-6

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	RG7440

Solubility (25°C) *	In vitro	DMSO	92 mg/mL (200.87 mM)
		Water	<1 mg/mL (
		Ethanol	92 mg/mL (200.87 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	(S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one

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Product Categories : PI3K/Akt/mTOR > Akt Inhibitor