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G1T38

Product Name
G1T38
CAS No.
1628256-23-4
Chemical Name
G1T38
Synonyms
G1T38;Lerociclib;G1T38 ，S8568;Lerociclib (G1T38);2'-((5-(4-Isopropylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one;7',8'-Dihydro-2'-[[5-[4-(1-methylethyl)-1-piperazinyl]-2-pyridinyl]amino]spiro[cyclohexane-1,9'(6'H)-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one;Spiro[cyclohexane-1,9'(6'H)-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one, 7',8'-dihydro-2'-[[5-[4-(1-methylethyl)-1-piperazinyl]-2-pyridinyl]amino]-
CBNumber
CB33335416
Molecular Formula
C26H34N8O
Formula Weight
474.6
MOL File
1628256-23-4.mol
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G1T38 Property

Density 
1.41±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:1.0(Max Conc. mg/mL);2.11(Max Conc. mM)
form 
Solid
pka
13.33±0.20(Predicted)
color 
Yellow to brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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G1T38 Chemical Properties,Usage,Production

Uses

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

in vivo

In this HER2+ breast cancer model, Mice treated with Lerociclib elicits 8% tumor regression after 21 days of treatment while control animals have a 577% increase in tumor burden over the same treatment period. Compared to the vehicle-treated mice, daily treatment with 100 mg/kg of Lerocyclib or palbociclib shows tumor regression within 10 days in the MCF7 xenograft model. After 27 days of treatment, tumor growth inhibition is observed in the 10, 50, and 100 mg/kg Lerociclib cohorts (approximately 12%, 74%, and 90% inhibition, respectively). Daily oral palbociclib treatment causes an 18%, 66%, and 87% tumor growth inhibition in the 10, 50, and 100 mg/kg dosage cohorts, respectively. Interestingly, at 50 mg/kg, Lerociclib is significantly more efficaciou than palbociclib. Similar results are seen in the ER+ZR-75-1 breast cancer xenograft model when comparing Lerocyclib and palbociclib at the 50 mg/kg dose. Lerociclib treated mice exhibits 77% TGI with an overall 60% tumor growth delay demonstrating Lerocyclib alone is highly efficacious in this NSCLC tumor model.

IC 50

cdk2/cyclin A: 1.5 μM (IC50); CDK2/cyclinE: 3.6 μM (IC50); Cdk4/cyclin D1: 1 nM (IC50); cdk6/cyclin D3: 2 nM (IC50); CDK9/Cyclin T: 28 nM (IC50); CDK5/p35: 0.832 μM (IC50); CDK1/cyclinB1: 2.4 μM (IC50); CDK7/Cyclin H/MAT1: 2.4 μM (IC50); Cdk5/p25: 1.2 μM (IC50)

References

[1] Bisi JE, et al. Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 2017 Jun 27;8(26):42343-42358. DOI:10.18632/oncotarget.16216

G1T38 Preparation Products And Raw materials

Raw materials

Preparation Products

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G1T38 Suppliers

China 46 United States 5 Global 51
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Country
China
ProdList
1077
Advantage
64
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9510
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4769
Advantage
55
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
ChengDu TongChuangYuan Pharmaceutical Co.Ltd
Tel
028-83379370 13880556291
Fax
028-87747383
Email
tcy@tcypharm.com
Country
China
ProdList
7218
Advantage
58
Shanghai SuperLan Chemcial Technique Centre
Tel
0-2022843681 15618226720
Fax
+86-21-51601218
Email
chaolaichem@foxmail.com
Country
China
ProdList
12475
Advantage
58
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Medi-tech Bioscientific Co., Ltd.
Tel
0519-83246372 13585352506
Fax
0519-83246372
Country
China
ProdList
1844
Advantage
58
Chuzhou KeMail Chemical Technology Co., Ltd
Tel
0550-5196001 15000891977
Fax
0550-5196001
Email
wj520wjxby@126.com
Country
China
ProdList
1944
Advantage
55

1628256-23-4, G1T38Related Search:


  • G1T38
  • Lerociclib
  • 7',8'-Dihydro-2'-[[5-[4-(1-methylethyl)-1-piperazinyl]-2-pyridinyl]amino]spiro[cyclohexane-1,9'(6'H)-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one
  • Lerociclib (G1T38)
  • Spiro[cyclohexane-1,9'(6'H)-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one, 7',8'-dihydro-2'-[[5-[4-(1-methylethyl)-1-piperazinyl]-2-pyridinyl]amino]-
  • 2'-((5-(4-Isopropylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one
  • G1T38 ，S8568
  • 1628256-23-4
  • C26H34N8O
  • APIS