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CCT128930

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CCT128930 Basic information

Product Name:
CCT128930
Synonyms:
  • 4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidin-4-aMine
  • CCT128930 (CCT 128930
  • CS-447
  • 4-[(4-Chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinamine
  • 4-PiperidinaMine, 4-[(4-chlorophenyl)Methyl]-1-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-
  • CCT128930, >=98%
  • CCT128930
  • 4-(4-Chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-ylamine
CAS:
885499-61-6
MF:
C18H20ClN5
MW:
341.84
Product Categories:
  • Akt
  • mTOR
  • PI3K
  • Inhibitors
Mol File:
885499-61-6.mol
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CCT128930 Chemical Properties

Density 
1.39
storage temp. 
Store at -20°C
solubility 
DMSO : 36.67 mg/mL (107.27 mM; Need ultrasonic)
form 
Powder
pka
13.93±0.50(Predicted)
color 
Off-white to yellow
InChI
InChI=1S/C18H20ClN5/c19-14-3-1-13(2-4-14)11-18(20)6-9-24(10-7-18)17-15-5-8-21-16(15)22-12-23-17/h1-5,8,12H,6-7,9-11,20H2,(H,21,22,23)
InChIKey
RZIDZIGAXXNODG-UHFFFAOYSA-N
SMILES
N1(C2N=CN=C3NC=CC3=2)CCC(CC2=CC=C(Cl)C=C2)(N)CC1
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Safety Information

HS Code 
2933399990
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CCT128930 Usage And Synthesis

Uses

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM.

Uses

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2.

in vivo

CCT128930 (25 or 40 mg/kg; i.p. daily or twice daily for 5 days) shows antitumor activities in U87MG and BT474 human breast cancer xenografts[1].
Summary of the pharmacokinetic parameters of CCT128930 (25 mg/kg) in CrTacNCr-Fox1nu mice[1]

TissueRouteT1/2
(h)		Tmax
(h)		Cmax
(μM)		Vss
(L)		Cl
(L/h)		AUC0-∞
(μMh)		 Bioavailability
(%)
Plasmai.v.0.950.083 6.36 0.25 0.325 4.62100
Plasmai.p.2.330.51.28N/A0.372 1.3328.8
Tumori.p.3.8918.02N/A0.06*25.8N/A
Plasmap.o.0.570.50.432N/A0.3170.3928.5

*Apparent clearance.
Animal Model:6-8 weeks old female CrTacNCr-Fox1nu mice[1]
Dosage:25 mg/kg (U87MG human glioblastoma xenografts) or 40 mg/kg (BT474 human breast cancer xenografts)
Administration:i.p. daily for 5 days (U87MG human glioblastoma xenografts); i.p. twice daily for 5 days (BT474 human breast cancer xenografts)
Result:Giving a treated:control (T/C) ratio on day 12 of 48%. There was no weight loss associated with this regime in U87MG human glioblastoma xenografts.
Had a profound antitumor effect with complete growth arrest and a T/C ratio of 29% on day 22. This regimen was associated with minimal weight loss, with a nadir of only 94.8% of the initial body weight on day 15 of treatment in BT474 human breast cancer xenografts.

target

Akt2

IC 50

Akt2: 6 nM (IC50); p70S6K: 120 nM (IC50); PKA: 168 nM (IC50); Autophagy; Apoptosis

CCT128930Supplier

Nantong Hi-Future Biotechnology Co., Ltd Gold
Tel
18051384581
Email
sales@chemhifuture.com
Shanghai Boyle Chemical Co., Ltd.
Tel
021-50182298 021-50180596
Email
sales@boylechem.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Email
sales@trio-pharmatech.com
Sphinx Scientific Laboratory (Tianjin) Co., Ltd.
Tel
022-66211289-843 13672102692
Email
contact@sphinxpharm.com
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