1. Cell Cycle/DNA Damage
  2. CDK
  3. CAN508

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.

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CAN508

CAN508 構造式

CAS 番号 : 140651-18-9

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 93 在庫あり
Solution
10 mM * 1 mL in DMSO USD 93 在庫あり
Solid
5 mg $85 在庫あり
10 mg $128 在庫あり
25 mg $256 在庫あり
50 mg $385 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

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  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity[1][2].

IC50 & Target[1]

CDK9/cyclinT1

0.35 μM (IC50)

CDK2/cyclinE

20 μM (IC50)

cdk2/cyclin A

69 μM (IC50)

Cdk4/cyclin D1

13.5 μM (IC50)

CDK7/cyclin H

26 μM (IC50)

Cdk1/cyclin B

44 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
786-0 GI50
26.2 μM
Compound: CAN508
Cytotoxicity against human 786-0 cells
Cytotoxicity against human 786-0 cells
[PMID: 21777997]
A498 GI50
18.2 μM
Compound: CAN508
Cytotoxicity against human A498 cells
Cytotoxicity against human A498 cells
[PMID: 21777997]
A549 GI50
22.5 μM
Compound: CAN508
Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
[PMID: 21777997]
ACHN GI50
15.6 μM
Compound: CAN508
Cytotoxicity against human ACHN cells
Cytotoxicity against human ACHN cells
[PMID: 21777997]
BT-549 GI50
14 μM
Compound: CAN508
Cytotoxicity against human BT549 cells
Cytotoxicity against human BT549 cells
[PMID: 21777997]
CAKI-1 GI50
14.8 μM
Compound: CAN508
Cytotoxicity against human Caki1 cells
Cytotoxicity against human Caki1 cells
[PMID: 21777997]
CCRF-CEM GI50
20 μM
Compound: CAN508
Cytotoxicity against human CCRF-CEM cells
Cytotoxicity against human CCRF-CEM cells
[PMID: 21777997]
COLO 205 GI50
18.9 μM
Compound: CAN508
Cytotoxicity against human COLO205 cells
Cytotoxicity against human COLO205 cells
[PMID: 21777997]
DU-145 GI50
17 μM
Compound: CAN508
Cytotoxicity against human DU145 cells
Cytotoxicity against human DU145 cells
[PMID: 21777997]
EKVX GI50
22 μM
Compound: CAN508
Cytotoxicity against human EKVX cells
Cytotoxicity against human EKVX cells
[PMID: 21777997]
G-361 IC50
64 μM
Compound: 31b, (CAN508)
Antiproliferative activity against G361 cell line
Antiproliferative activity against G361 cell line
[PMID: 17064068]
HCC 2998 GI50
29.4 μM
Compound: CAN508
Cytotoxicity against human HCC2998 cells
Cytotoxicity against human HCC2998 cells
[PMID: 21777997]
HCT-116 GI50
18.9 μM
Compound: CAN508
Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
[PMID: 21777997]
HCT-15 GI50
24.2 μM
Compound: CAN508
Cytotoxicity against human HCT15 cells
Cytotoxicity against human HCT15 cells
[PMID: 21777997]
HL-60(TB) GI50
6.4 μM
Compound: CAN508
Cytotoxicity against human HL-60(TB) cells
Cytotoxicity against human HL-60(TB) cells
[PMID: 21777997]
HMEC-1 IC50
20 μM
Compound: CAN508
Inhibition of RNA synthesis in human HMEC1 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
Inhibition of RNA synthesis in human HMEC1 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
[PMID: 21777997]
HOP-62 GI50
31.8 μM
Compound: CAN508
Cytotoxicity against human HOP62 cells
Cytotoxicity against human HOP62 cells
[PMID: 21777997]
HOP-92 GI50
18.2 μM
Compound: CAN508
Cytotoxicity against human HOP92 cells
Cytotoxicity against human HOP92 cells
[PMID: 21777997]
HOS IC50
49 μM
Compound: 31b, (CAN508)
Antiproliferative activity against HOS cell line
Antiproliferative activity against HOS cell line
[PMID: 17064068]
HT-29 GI50
29.7 μM
Compound: CAN508
Cytotoxicity against human HT-29 cells
Cytotoxicity against human HT-29 cells
[PMID: 21777997]
Hs-578T GI50
21.8 μM
Compound: CAN508
Cytotoxicity against human Hs 578T cells
Cytotoxicity against human Hs 578T cells
[PMID: 21777997]
IGROV-1 GI50
20.6 μM
Compound: CAN508
Cytotoxicity against human IGROV1 cells
Cytotoxicity against human IGROV1 cells
[PMID: 21777997]
K562 GI50
9.2 μM
Compound: CAN508
Cytotoxicity against human K562 cells
Cytotoxicity against human K562 cells
[PMID: 21777997]
K562 IC50
33 μM
Compound: IIIa, CAN508
Cytotoxicity against human K562 cells after 72 hrs by calcein AM staining-based fluorescence assay
Cytotoxicity against human K562 cells after 72 hrs by calcein AM staining-based fluorescence assay
[PMID: 25835357]
K562 IC50
62 μM
Compound: 31b, (CAN508)
Antiproliferative activity against K562 cell line
Antiproliferative activity against K562 cell line
[PMID: 17064068]
KM12 GI50
17.1 μM
Compound: CAN508
Cytotoxicity against human KM12 cells
Cytotoxicity against human KM12 cells
[PMID: 21777997]
LOX IMVI GI50
4.1 μM
Compound: CAN508
Cytotoxicity against human LOXIMVI cells
Cytotoxicity against human LOXIMVI cells
[PMID: 21777997]
M14 GI50
15.9 μM
Compound: CAN508
Cytotoxicity against human M14 cells
Cytotoxicity against human M14 cells
[PMID: 21777997]
MCF7 GI50
23.5 μM
Compound: CAN508
Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
[PMID: 21777997]
MCF7 IC50
15 μM
Compound: CAN508
Inhibition of RNA synthesis in human MCF7 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
Inhibition of RNA synthesis in human MCF7 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
[PMID: 21777997]
MCF7 IC50
33 μM
Compound: 31b, (CAN508)
Antiproliferative activity against MCF7 cell line
Antiproliferative activity against MCF7 cell line
[PMID: 17064068]
MCF7 IC50
62 μM
Compound: IIIa, CAN508
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM staining-based fluorescence assay
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM staining-based fluorescence assay
[PMID: 25835357]
MDA-MB-231 GI50
16.7 μM
Compound: CAN508
Cytotoxicity against human MDA-MB-231 cells
Cytotoxicity against human MDA-MB-231 cells
[PMID: 21777997]
MDA-MB-435 GI50
17.1 μM
Compound: CAN508
Cytotoxicity against human MDA-MB-435 cells
Cytotoxicity against human MDA-MB-435 cells
[PMID: 21777997]
MOLT-4 GI50
13.5 μM
Compound: CAN508
Cytotoxicity against human MOLT4 cells
Cytotoxicity against human MOLT4 cells
[PMID: 21777997]
Malme-3M GI50
24.5 μM
Compound: CAN508
Cytotoxicity against human MALME-3M cells
Cytotoxicity against human MALME-3M cells
[PMID: 21777997]
NCI-H226 GI50
17.7 μM
Compound: CAN508
Cytotoxicity against human NCI-H226 cells
Cytotoxicity against human NCI-H226 cells
[PMID: 21777997]
NCI-H23 GI50
19.1 μM
Compound: CAN508
Cytotoxicity against human NCI-H23 cells
Cytotoxicity against human NCI-H23 cells
[PMID: 21777997]
NCI-H322M GI50
25.1 μM
Compound: CAN508
Cytotoxicity against human NCI-H322M cells
Cytotoxicity against human NCI-H322M cells
[PMID: 21777997]
NCI-H460 GI50
25.1 μM
Compound: CAN508
Cytotoxicity against human NCI-H460 cells
Cytotoxicity against human NCI-H460 cells
[PMID: 21777997]
NCI-H522 GI50
24.3 μM
Compound: CAN508
Cytotoxicity against human NCI-H522 cells
Cytotoxicity against human NCI-H522 cells
[PMID: 21777997]
NCI/ADR-RES GI50
22.5 μM
Compound: CAN508
Cytotoxicity against human NCI/ADR-RES cells
Cytotoxicity against human NCI/ADR-RES cells
[PMID: 21777997]
OVCAR-3 GI50
22.8 μM
Compound: CAN508
Cytotoxicity against human OVCAR3 cells
Cytotoxicity against human OVCAR3 cells
[PMID: 21777997]
OVCAR-4 GI50
19 μM
Compound: CAN508
Cytotoxicity against human OVCAR4 cells
Cytotoxicity against human OVCAR4 cells
[PMID: 21777997]
OVCAR-5 GI50
23.5 μM
Compound: CAN508
Cytotoxicity against human OVCAR5 cells
Cytotoxicity against human OVCAR5 cells
[PMID: 21777997]
OVCAR-8 GI50
18 μM
Compound: CAN508
Cytotoxicity against human OVCAR8 cells
Cytotoxicity against human OVCAR8 cells
[PMID: 21777997]
PC-3 GI50
20.3 μM
Compound: CAN508
Cytotoxicity against human PC3 cells
Cytotoxicity against human PC3 cells
[PMID: 21777997]
RPMI-8226 GI50
14.4 μM
Compound: CAN508
Cytotoxicity against human RPMI8226 cells
Cytotoxicity against human RPMI8226 cells
[PMID: 21777997]
RPMI-8226 IC50
24.9 μM
Compound: IIIa, CAN508
Cytotoxicity against human RPMI8226 cells after 72 hrs by calcein AM staining-based fluorescence assay
Cytotoxicity against human RPMI8226 cells after 72 hrs by calcein AM staining-based fluorescence assay
[PMID: 25835357]
RXF 393 GI50
18.4 μM
Compound: CAN508
Cytotoxicity against human RXF393 cells
Cytotoxicity against human RXF393 cells
[PMID: 21777997]
SF-268 GI50
20.6 μM
Compound: CAN508
Cytotoxicity against human SF268 cells
Cytotoxicity against human SF268 cells
[PMID: 21777997]
SF-295 GI50
23.3 μM
Compound: CAN508
Cytotoxicity against human SF295 cells
Cytotoxicity against human SF295 cells
[PMID: 21777997]
SF-539 GI50
13.2 μM
Compound: CAN508
Cytotoxicity against human SF539 cells
Cytotoxicity against human SF539 cells
[PMID: 21777997]
SK-MEL-2 GI50
14.4 μM
Compound: CAN508
Cytotoxicity against human SK-MEL-2 cells
Cytotoxicity against human SK-MEL-2 cells
[PMID: 21777997]
SK-MEL-28 GI50
22.1 μM
Compound: CAN508
Cytotoxicity against human SK-MEL-28 cells
Cytotoxicity against human SK-MEL-28 cells
[PMID: 21777997]
SK-MEL-5 GI50
13.9 μM
Compound: CAN508
Cytotoxicity against human SK-MEL-5 cells
Cytotoxicity against human SK-MEL-5 cells
[PMID: 21777997]
SK-OV-3 GI50
49.2 μM
Compound: CAN508
Cytotoxicity against human SKOV3 cells
Cytotoxicity against human SKOV3 cells
[PMID: 21777997]
SN12C GI50
23.3 μM
Compound: CAN508
Cytotoxicity against human SN12C cells
Cytotoxicity against human SN12C cells
[PMID: 21777997]
SNB-19 GI50
29.9 μM
Compound: CAN508
Cytotoxicity against human SNB19 cells
Cytotoxicity against human SNB19 cells
[PMID: 21777997]
SNB-75 GI50
18.5 μM
Compound: CAN508
Cytotoxicity against human SNB75 cells
Cytotoxicity against human SNB75 cells
[PMID: 21777997]
SR GI50
10.3 μM
Compound: CAN508
Cytotoxicity against human SR cells
Cytotoxicity against human SR cells
[PMID: 21777997]
SW-620 GI50
26.3 μM
Compound: CAN508
Cytotoxicity against human SW620 cells
Cytotoxicity against human SW620 cells
[PMID: 21777997]
Sf9 IC50
0.35 μM
Compound: IIIa, CAN508
Inhibition of CDK9/cyclin T1 (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK9/cyclin T1 (unknown origin) expressed in baculovirus infected Sf9 cells
[PMID: 25835357]
Sf9 IC50
13.5 μM
Compound: IIIa, CAN508
Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected Sf9 cells
[PMID: 25835357]
Sf9 IC50
20 μM
Compound: IIIa, CAN508
Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf9 cells
[PMID: 25835357]
Sf9 IC50
26 μM
Compound: IIIa, CAN508
Inhibition of CDK7/cyclin H (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK7/cyclin H (unknown origin) expressed in baculovirus infected Sf9 cells
[PMID: 25835357]
Sf9 IC50
44 μM
Compound: IIIa, CAN508
Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 cells
[PMID: 25835357]
T47D GI50
14.2 μM
Compound: CAN508
Cytotoxicity against human T47D cells
Cytotoxicity against human T47D cells
[PMID: 21777997]
TK-10 GI50
25.6 μM
Compound: CAN508
Cytotoxicity against human TK10 cells
Cytotoxicity against human TK10 cells
[PMID: 21777997]
U-251 GI50
21.2 μM
Compound: CAN508
Cytotoxicity against human U251 cells
Cytotoxicity against human U251 cells
[PMID: 21777997]
UACC-257 GI50
24.4 μM
Compound: CAN508
Cytotoxicity against human UACC257 cells
Cytotoxicity against human UACC257 cells
[PMID: 21777997]
UACC-62 GI50
11 μM
Compound: CAN508
Cytotoxicity against human UACC62 cells
Cytotoxicity against human UACC62 cells
[PMID: 21777997]
UO-31 GI50
13.7 μM
Compound: CAN508
Cytotoxicity against human UO31 cells
Cytotoxicity against human UO31 cells
[PMID: 21777997]
体外実験

CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays[1].
CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC50s ranging from 34.99 to 91.09 μM[2].
CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: SKGT4, OE33 and FLO-1 cells
Concentration: 40 μM
Incubation Time: 72 hours
Result: Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls.
体内実験

CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts)[1]
Dosage: 60 mg/kg
Administration: I.p.; daily for 10 days
Result: Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.
分子量

218.22

分子式

C9H10N6O

CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=CC=C(/N=N/C2=C(N)NN=C2N)C=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : 250 mg/mL (1145.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5825 mL 22.9127 mL 45.8253 mL
5 mM 0.9165 mL 4.5825 mL 9.1651 mL
10 mM 0.4583 mL 2.2913 mL 4.5825 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

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体積 (開始)

V1

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (9.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.5825 mL 22.9127 mL 45.8253 mL 114.5633 mL
5 mM 0.9165 mL 4.5825 mL 9.1651 mL 22.9127 mL
10 mM 0.4583 mL 2.2913 mL 4.5825 mL 11.4563 mL
15 mM 0.3055 mL 1.5275 mL 3.0550 mL 7.6376 mL
20 mM 0.2291 mL 1.1456 mL 2.2913 mL 5.7282 mL
25 mM 0.1833 mL 0.9165 mL 1.8330 mL 4.5825 mL
30 mM 0.1528 mL 0.7638 mL 1.5275 mL 3.8188 mL
40 mM 0.1146 mL 0.5728 mL 1.1456 mL 2.8641 mL
50 mM 0.0917 mL 0.4583 mL 0.9165 mL 2.2913 mL
60 mM 0.0764 mL 0.3819 mL 0.7638 mL 1.9094 mL
80 mM 0.0573 mL 0.2864 mL 0.5728 mL 1.4320 mL
100 mM 0.0458 mL 0.2291 mL 0.4583 mL 1.1456 mL
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
CAN508
製品番号:
HY-100429
数量:
MCE 日本正規代理店: